Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38.
Plasmodium
bioinformatics
database
drug discovery
malaria
molecular target
Journal
British journal of pharmacology
ISSN: 1476-5381
Titre abrégé: Br J Pharmacol
Pays: England
ID NLM: 7502536
Informations de publication
Date de publication:
08 2023
08 2023
Historique:
revised:
10
05
2023
received:
20
05
2022
accepted:
14
05
2023
medline:
7
7
2023
pubmed:
18
5
2023
entrez:
17
5
2023
Statut:
ppublish
Résumé
Antimalarial drug discovery has until recently been driven by high-throughput phenotypic cellular screening, allowing millions of compounds to be assayed and delivering clinical drug candidates. In this review, we will focus on target-based approaches, describing recent advances in our understanding of druggable targets in the malaria parasite. Targeting multiple stages of the Plasmodium lifecycle, rather than just the clinically symptomatic asexual blood stage, has become a requirement for new antimalarial medicines, and we link pharmacological data clearly to the parasite stages to which it applies. Finally, we highlight the IUPHAR/MMV Guide to MALARIA PHARMACOLOGY, a web resource developed for the malaria research community that provides open and optimized access to published data on malaria pharmacology.
Substances chimiques
Antimalarials
0
Types de publication
Journal Article
Review
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1899-1929Informations de copyright
© 2023 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.
Références
Adachi, R., Okada, K., Skene, R., Ogawa, K., Miwa, M., Tsuchinaga, K., Ohkubo, S., Henta, T., & Kawamoto, T. (2017). Discovery of a novel prolyl-tRNA synthetase inhibitor and elucidation of its binding mode to the ATP site in complex with l-proline. Biochemical and Biophysical Research Communications, 488(2), 393-399. https://doi.org/10.1016/j.bbrc.2017.05.064
Adderley, J., & Doerig, C. (2022). Comparative analysis of the kinomes of Plasmodium falciparum, Plasmodium vivax and their host Homo sapiens. BMC Genomics, 23(1), 237. https://doi.org/10.1186/s12864-022-08457-0
Adderley, J., Williamson, T., & Doerig, C. (2021). Parasite and host erythrocyte kinomics of Plasmodium infection. Trends in Parasitology, 37(6), 508-524. https://doi.org/10.1016/j.pt.2021.01.002
Alam, M. M., Sanchez-Azqueta, A., Janha, O., Flannery, E. L., Mahindra, A., Mapesa, K., Char, A. B., Sriranganadane, D., Brancucci, N. M. B., Antonova-Koch, Y., Crouch, K., Simwela, N. V., Millar, S. B., Akinwale, J., Mitcheson, D., Solyakov, L., Dudek, K., Jones, C., Zapatero, C., … Tobin, A. B. (2019). Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science (New York, N.Y.), 365(6456), eaau1682. https://doi.org/10.1126/science.aau1682
Alam, M. M., Solyakov, L., Bottrill, A. R., Flueck, C., Siddiqui, F. A., Singh, S., Mistry, S., Viskaduraki, M., Lee, K., Hopp, C. S., Chitnis, C. E., Doerig, C., Moon, R. W., Green, J. L., Holder, A. A., Baker, D. A., & Tobin, A. B. (2015). Phosphoproteomics reveals malaria parasite protein kinase G as a signalling hub regulating egress and invasion. Nature Communications, 6, 7285. https://doi.org/10.1038/ncomms8285
Aleshnick, M., Ganusov, V. V., Nasir, G., Yenokyan, G., & Sinnis, P. (2020). Experimental determination of the force of malaria infection reveals a non-linear relationship to mosquito sporozoite loads. PLoS Pathogens, 16(5), e1008181. https://doi.org/10.1371/journal.ppat.1008181
Anderson, A. C. (2005). Targeting DHFR in parasitic protozoa. Drug Discovery Today, 10(2), 121-128. https://doi.org/10.1016/S1359-6446(04)03308-2
Anusha, S., Sinha, A., Babu Rajeev, C. P., Chu, T. T. T., Mathai, J., Ximei, H., Fuchs, J. E., Shivananju, N., Bender, A., Preiser, P. R., Rangappa, K. S., Basappa, S., & Chandramohanadas, R. (2015). Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials. Organic & Biomolecular Chemistry, 13(43), 10681-10690. https://doi.org/10.1039/c5ob01479d
Arendse, L. B., Murithi, J. M., Qahash, T., Pasaje, C. F. A., Godoy, L. C., Dey, S., Gibhard, L., Ghidelli-Disse, S., Drewes, G., Bantscheff, M., Lafuente-Monasterio, M. J., Fienberg, S., Wambua, L., Gachuhi, S., Coertzen, D., van der Watt, M., Reader, J., Aswat, A. S., Erlank, E., … Chibale, K. (2022). The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages. Science Translational Medicine, 14(667), eabo7219. https://doi.org/10.1126/scitranslmed.abo7219
Arendse, L. B., Wyllie, S., Chibale, K., & Gilbert, I. H. (2021). Plasmodium kinases as potential drug targets for malaria: Challenges and opportunities. ACS Infectious Diseases, 7(3), 518-534. https://doi.org/10.1021/acsinfecdis.0c00724
Arendt, C. S., & Hochstrasser, M. (1997). Identification of the yeast 20S proteasome catalytic centers and subunit interactions required for active-site formation. Proceedings of the National Academy of Sciences of the United States of America, 94(14), 7156-7161. https://doi.org/10.1073/pnas.94.14.7156
Armstrong, J. F., Faccenda, E., Harding, S. D., Pawson, A. J., Southan, C., Sharman, J. L., Campo, B., Cavanagh, D. R., Alexander, S. P. H., Davenport, A. P., Spedding, M., Davies, J. A., & NC-IUPHAR. (2020). The IUPHAR/BPS guide to PHARMACOLOGY in 2020: Extending immunopharmacology content and introducing the IUPHAR/MMV guide to MALARIA PHARMACOLOGY. Nucleic Acids Research, 48(D1), D1006-D1021. https://doi.org/10.1093/nar/gkz951
Aurrecoechea, C., Brestelli, J., Brunk, B. P., Dommer, J., Fischer, S., Gajria, B., Gao, X., Gingle, A., Grant, G., Harb, O. S., Heiges, M., Innamorato, F., Iodice, J., Kissinger, J. C., Kraemer, E., Li, W., Miller, J. A., Nayak, V., Pennington, C., … Wang, H. (2009). PlasmoDB: A functional genomic database for malaria parasites. Nucleic Acids Research, 37(Database issue), D539-D543. https://doi.org/10.1093/nar/gkn814
Baker, D. A., Matralis, A. N., Osborne, S. A., Large, J. M., & Penzo, M. (2020). Targeting the malaria parasite cGMP-dependent protein kinase to develop new drugs. Frontiers in Microbiology, 11, 602803. https://doi.org/10.3389/fmicb.2020.602803
Baker, D. A., Stewart, L. B., Large, J. M., Bowyer, P. W., Ansell, K. H., Jiménez-Díaz, M. B., El Bakkouri, M., Birchall, K., Dechering, K. J., Bouloc, N. S., Coombs, P. J., Whalley, D., Harding, D. J., Smiljanic-Hurley, E., Wheldon, M. C., Walker, E. M., Dessens, J. T., Lafuente, M. J. J., Sanz, L. M., … Osborne, S. A. (2017). A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission. Nature Communications, 8(1), 430. http://view.ncbi.nlm.nih.gov/pubmed/28874661
Baragaña, B., Hallyburton, I., Lee, M. C., Norcross, N. R., Grimaldi, R., Otto, T. D., Proto, W. R., Blagborough, A. M., Meister, S., Wirjanata, G., Ruecker, A., Upton, L. M., Abraham, T. S., Almeida, M. J., Pradhan, A., Porzelle, A., Martínez, M. S. S., Bolscher, J. M., Woodland, A., … Gilbert, I. H. (2015). A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature, 522(7556), 315-320.
Barata, L., Houzé, P., Boutbibe, K., Zanghi, G., Franetich, J.-F., Mazier, D., & Clain, J. (2016). In vitro analysis of the interaction between atovaquone and proguanil against liver stage malaria parasites. Antimicrobial Agents and Chemotherapy, 60(7), 4333-4335. https://doi.org/10.1128/AAC.01685-15
Bell, A. S., Mills, J. E., Williams, G. P., Brannigan, J. A., Wilkinson, A. J., Parkinson, T., Leatherbarrow, R. J., Tate, E. W., Holder, A. A., & Smith, D. F. (2012). Selective inhibitors of protozoan protein N-myristoyltransferases as starting points for tropical disease medicinal chemistry programs. PLoS Neglected Tropical Diseases, 6(4), e1625. https://doi.org/10.1371/journal.pntd.0001625
Bhatt, S., Weiss, D. J., Cameron, E., Bisanzio, D., Mappin, B., Dalrymple, U., Battle, K., Moyes, C. L., Henry, A., Eckhoff, P. A., Wenger, E. A., Briët, O., Penny, M. A., Smith, T. A., Bennett, A., Yukich, J., Eisele, T. P., Griffin, J. T., Fergus, C. A., … Gething, P. W. (2015). The effect of malaria control on Plasmodium falciparum in Africa between 2000 and 2015. Nature, 526(7572), 207-211. https://doi.org/10.1038/nature15535
Bhatt, T. K., Kapil, C., Khan, S., Jairajpuri, M. A., Sharma, V., Santoni, D., Silvestrini, F., Pizzi, E., & Sharma, A. (2009). A genomic glimpse of aminoacyl-tRNA synthetases in malaria parasite Plasmodium falciparum. BMC Genomics, 10, 644. https://doi.org/10.1186/1471-2164-10-644
Bienroth, S., Wahle, E., Suter-Crazzolara, C., & Keller, W. (1991). Purification of the cleavage and polyadenylation factor involved in the 3′-processing of messenger RNA precursors. The Journal of Biological Chemistry, 266(29), 19768-19776.
Birkholtz, L.-M., Coetzer, T. L., Mancama, D., Leroy, D., & Alano, P. (2016). Discovering new transmission-blocking antimalarial compounds: Challenges and opportunities. Trends in Parasitology, 32(9), 669-681. https://doi.org/10.1016/j.pt.2016.04.017
Birth, D., Kao, W.-C., & Hunte, C. (2014). Structural analysis of atovaquone-inhibited cytochrome bc1 complex reveals the molecular basis of antimalarial drug action. Nature Communications, 5, 4029. https://doi.org/10.1038/ncomms5029
Blake, L. D., Johnson, M. E., Siegel, S. V., McQueen, A., Iyamu, I. D., Shaikh, A. K., Shultis, M. W., Manetsch, R., & Kyle, D. E. (2017). Menoctone resistance in malaria parasites is conferred by M133I mutations in cytochrome b that are transmissible through mosquitoes. Antimicrobial Agents and Chemotherapy, 61(8), e00689. https://doi.org/10.1128/AAC.00689-17
Boddey, J. A., Hodder, A. N., Günther, S., Gilson, P. R., Patsiouras, H., Kapp, E. A., Pearce, J. A., de Koning-Ward, T. F., Simpson, R. J., Crabb, B. S., & Cowman, A. F. (2010). An aspartyl protease directs malaria effector proteins to the host cell. Nature, 463(7281), 627-631. https://doi.org/10.1038/nature08728
Bolscher, J. M., Koolen, K. M. J., van Gemert, G. J., van de Vegte-Bolmer, M. G., Bousema, T., Leroy, D., Sauerwein, R. W., & Dechering, K. J. (2015). A combination of new screening assays for prioritization of transmission-blocking antimalarials reveals distinct dynamics of marketed and experimental drugs. The Journal of Antimicrobial Chemotherapy, 70(5), 1357-1366. https://doi.org/10.1093/jac/dkv003
Booker, M. L., Bastos, C. M., Kramer, M. L., Barker, R. H., Skerlj, R., Sidhu, A. B., Deng, X., Celatka, C., Cortese, J. F., Guerrero Bravo, J. E., Crespo Llado, K. N., Serrano, A. E., Angulo-Barturen, I., Jiménez-Díaz, M. B., Viera, S., Garuti, H., Wittlin, S., Papastogiannidis, P., Lin, J.-W., … Sybertz, E. (2010). Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model. The Journal of Biological Chemistry, 285(43), 33054-33064. https://doi.org/10.1074/jbc.M110.162081
Boonyalai, N., Collins, C. R., Hackett, F., Withers-Martinez, C., & Blackman, M. J. (2018). Essentiality of Plasmodium falciparum plasmepsin V. PLoS ONE, 13(12), e0207621. https://doi.org/10.1371/journal.pone.0207621
Boutin, J. A. (1997). Myristoylation. Cellular Signalling, 9(1), 15-35. https://doi.org/10.1016/s0898-6568(96)00100-3
Bowman, J. D., Merino, E. F., Brooks, C. F., Striepen, B., Carlier, P. R., & Cassera, M. B. (2014). Antiapicoplast and gametocytocidal screening to identify the mechanisms of action of compounds within the malaria box. Antimicrobial Agents and Chemotherapy, 58(2), 811-819. https://doi.org/10.1128/AAC.01500-13
Bowyer, P. W., Gunaratne, R. S., Grainger, M., Withers-Martinez, C., Wickramsinghe, S. R., Tate, E. W., Leatherbarrow, R. J., Brown, K. A., Holder, A. A., & Smith, D. F. (2007). Molecules incorporating a benzothiazole core scaffold inhibit the N-myristoyltransferase of Plasmodium falciparum. The Biochemical Journal, 408(2), 173-180. https://doi.org/10.1042/BJ20070692
Boysen, K. E., & Matuschewski, K. (2011). Arrested oocyst maturation in Plasmodium parasites lacking type II NADH:ubiquinone dehydrogenase. The Journal of Biological Chemistry, 286(37), 32661-32671. https://doi.org/10.1074/jbc.M111.269399
Brochet, M., Collins, M. O., Smith, T. K., Thompson, E., Sebastian, S., Volkmann, K., Schwach, F., Chappell, L., Gomes, A. R., Berriman, M., Rayner, J. C., Baker, D. A., Choudhary, J., & Billker, O. (2014). Phosphoinositide metabolism links cGMP-dependent protein kinase G to essential Ca2+ signals at key decision points in the life cycle of malaria parasites. PLoS Biology, 12(3), e1001806. https://doi.org/10.1371/journal.pbio.1001806
Brunschwig, C., Lawrence, N., Taylor, D., Abay, E., Njoroge, M., Basarab, G. S., Le Manach, C., Paquet, T., Cabrera, D. G., Nchinda, A. T., de Kock, C., Wiesner, L., Denti, P., Waterson, D., Blasco, B., Leroy, D., Witty, M. J., Donini, C., Duffy, J., … Chibale, K. (2018). UCT943, a next-generation Plasmodium falciparum PI4K inhibitor preclinical candidate for the treatment of malaria. Antimicrobial Agents and Chemotherapy, 62(9), e00012-18. https://doi.org/10.1128/AAC.00012-18
Buchholz, K., Burke, T. A., Williamson, K. C., Wiegand, R. C., Wirth, D. F., & Marti, M. (2011). A high-throughput screen targeting malaria transmission stages opens new avenues for drug development. The Journal of Infectious Diseases, 203(10), 1445-1453. https://doi.org/10.1093/infdis/jir037
Bueno, J. M., Herreros, E., Angulo-Barturen, I., Ferrer, S., Fiandor, J. M., Gamo, F. J., Gargallo-Viola, D., & Derimanov, G. (2012). Exploration of 4(1H)-pyridones as a novel family of potent antimalarial inhibitors of the plasmodial cytochrome bc1. Future Medicinal Chemistry, 4(18), 2311-2323. https://doi.org/10.4155/fmc.12.177
Burrows, J., Fidock, D. A., Miller, R. S., & Rees, S. (2019). Blocking Plasmodium development in mosquitoes: A powerful new approach for expanding malaria control efforts. The American Journal of Tropical Medicine and Hygiene, 101(4), 734-735. https://doi.org/10.4269/ajtmh.19-0318
Burrows, J. N., Duparc, S., Gutteridge, W. E., Hooft van Huijsduijnen, R., Kaszubska, W., Macintyre, F., Mazzuri, S., Möhrle, J. J., & Wells, T. N. C. (2017). New developments in anti-malarial target candidate and product profiles. Malaria Journal, 16(1), 26. https://doi.org/10.1186/s12936-016-1675-x
Burrows, J. N., van Huijsduijnen, R. H., Möhrle, J. J., Oeuvray, C., & Wells, T. N. C. (2013). Designing the next generation of medicines for malaria control and eradication. Malaria Journal, 12, 187. https://doi.org/10.1186/1475-2875-12-187
Bushell, E., Gomes, A. R., Sanderson, T., Anar, B., Girling, G., Herd, C., Metcalf, T., Modrzynska, K., Schwach, F., Martin, R. E., Mather, M. W., McFadden, G. I., Parts, L., Rutledge, G. G., Vaidya, A. B., Wengelnik, K., Rayner, J. C., & Billker, O. (2017). Functional profiling of a Plasmodium genome reveals an abundance of essential genes. Cell, 170(2), 260-272.e8. https://doi.org/10.1016/j.cell.2017.06.030
Canfield, C. J., Milhous, W. K., Ager, A. L., Rossan, R. N., Sweeney, T. R., Lewis, N. J., & Jacobus, D. P. (1993). PS-15: A potent, orally active antimalarial from a new class of folic acid antagonists. The American Journal of Tropical Medicine and Hygiene, 49(1), 121-126. https://doi.org/10.4269/ajtmh.1993.49.121
Capper, M. J., O'Neill, P. M., Fisher, N., Strange, R. W., Moss, D., Ward, S. A., Berry, N. G., Lawrenson, A. S., Hasnain, S. S., Biagini, G. A., & Antonyuk, S. V. (2015). Antimalarial 4(1H)-pyridones bind to the Qi site of cytochrome bc1. Proceedings of the National Academy of Sciences of the United States of America, 112(3), 755-760. https://doi.org/10.1073/pnas.1416611112
Casewell, M. W., & Hill, R. L. (1987). Mupirocin (‘pseudomonic acid’)-A promising new topical antimicrobial agent. The Journal of Antimicrobial Chemotherapy, 19(1), 1-5. https://doi.org/10.1093/jac/19.1.1
Cha, S.-J., Park, K., Srinivasan, P., Schindler, C. W., van Rooijen, N., Stins, M., & Jacobs-Lorena, M. (2015). CD68 acts as a major gateway for malaria sporozoite liver infection. The Journal of Experimental Medicine, 212(9), 1391-1403. https://doi.org/10.1084/jem.20110575
Chaal, B. K., Gupta, A. P., Wastuwidyaningtyas, B. D., Luah, Y.-H., & Bozdech, Z. (2010). Histone deacetylases play a major role in the transcriptional regulation of the Plasmodium falciparum life cycle. PLoS Pathogens, 6(1), e1000737. https://doi.org/10.1371/journal.ppat.1000737
Chaliotis, A., Vlastaridis, P., Mossialos, D., Ibba, M., Becker, H. D., Stathopoulos, C., & Amoutzias, G. D. (2017). The complex evolutionary history of aminoacyl-tRNA synthetases. Nucleic Acids Research, 45(3), 1059-1068. https://doi.org/10.1093/nar/gkw1182
Cheuka, P. M., Centani, L., Arendse, L. B., Fienberg, S., Wambua, L., Renga, S. S., Dziwornu, G. A., Kumar, M., Lawrence, N., Taylor, D., Wittlin, S., Coertzen, D., Reader, J., van der Watt, M., Birkholtz, L.-M., & Chibale, K. (2021). New amidated 3,6-diphenylated imidazopyridazines with potent antiplasmodium activity are dual inhibitors of Plasmodium phosphatidylinositol-4-kinase and cGMP-dependent protein kinase. ACS Infectious Diseases, 7(1), 34-46. https://doi.org/10.1021/acsinfecdis.0c00481
Chiodini, P. L., Conlon, C. P., Hutchinson, D. B., Farquhar, J. A., Hall, A. P., Peto, T. E., Birley, H., & Warrell, D. A. (1995). Evaluation of atovaquone in the treatment of patients with uncomplicated Plasmodium falciparum malaria. The Journal of Antimicrobial Chemotherapy, 36(6), 1073-1078. https://doi.org/10.1093/jac/36.6.1073
Chua, M. J., Arnold, M. S. J., Xu, W., Lancelot, J., Lamotte, S., Späth, G. F., Prina, E., Pierce, R. J., Fairlie, D. P., Skinner-Adams, T. S., & Andrews, K. T. (2017). Effect of clinically approved HDAC inhibitors on Plasmodium, Leishmania and Schistosoma parasite growth. International Journal for Parasitology: Drugs and Drug Resistance, 7(1), 42-50. https://doi.org/10.1016/j.ijpddr.2016.12.005
Chua, M. J., Robaa, D., Skinner-Adams, T. S., Sippl, W., & Andrews, K. T. (2018). Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites. International Journal for Parasitology: Drugs and Drug Resistance, 8(2), 189-193. https://doi.org/10.1016/j.ijpddr.2018.03.001
Chughlay, M. F., El Gaaloul, M., Donini, C., Campo, B., Berghmans, P.-J., Lucardie, A., Marx, M. W., Cherkaoui-Rbati, M. H., Langdon, G., Angulo-Barturen, I., Viera, S., Rosanas-Urgell, A., Van Geertruyden, J.-P., & Chalon, S. (2021). Chemoprotective antimalarial activity of P218 against Plasmodium falciparum: A randomized, placebo-controlled volunteer infection study. The American Journal of Tropical Medicine and Hygiene, 104, 1348-1358. https://doi.org/10.4269/ajtmh.20-1165
Churcher, T. S., Sinden, R. E., Edwards, N. J., Poulton, I. D., Rampling, T. W., Brock, P. M., Griffin, J. T., Upton, L. M., Zakutansky, S. E., Sala, K. A., Angrisano, F., Hill, A. V. S., & Blagborough, A. M. (2017). Probability of transmission of malaria from mosquito to human is regulated by mosquito parasite density in naïve and vaccinated hosts. PLoS Pathogens, 13(1), e1006108. https://doi.org/10.1371/journal.ppat.1006108
Coleman, B. I., Skillman, K. M., Jiang, R. H. Y., Childs, L. M., Altenhofen, L. M., Ganter, M., Leung, Y., Goldowitz, I., Kafsack, B. F. C., Marti, M., Llinás, M., Buckee, C. O., & Duraisingh, M. T. (2014). A Plasmodium falciparum histone deacetylase regulates antigenic variation and gametocyte conversion. Cell Host & Microbe, 16(2), 177-186. https://doi.org/10.1016/j.chom.2014.06.01
Coteron, J. M., Marco, M., Esquivias, J., Deng, X., White, K. L., White, J., Koltun, M., El Mazouni, F., Kokkonda, S., Katneni, K., Bhamidipati, R., Shackleford, D. M., Angulo-Barturen, I., Ferrer, S. B., Jiménez-Díaz, M. B. B., Gamo, F.-J. J., Goldsmith, E. J., Charman, W. N., Bathurst, I., … Phillips, M. A. (2011). Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential. Journal of Medicinal Chemistry, 54(15), 5540-5561. https://doi.org/10.1021/jm200592f
Coux, O., Tanaka, K., & Goldberg, A. L. (1996). Structure and functions of the 20S and 26S proteasomes. Annual Review of Biochemistry, 65, 801-847. https://doi.org/10.1146/annurev.bi.65.070196.004101
Croft, A. M. (2007). A lesson learnt: The rise and fall of Lariam and Halfan. Journal of the Royal Society of Medicine, 100(4), 170-174. https://doi.org/10.1177/014107680710011411
Crowther, G. J., Napuli, A. J., Gilligan, J. H., Gagaring, K., Borboa, R., Francek, C., Chen, Z., Dagostino, E. F., Stockmyer, J. B., Wang, Y., Rodenbough, P. P., Castaneda, L. J., Leibly, D. J., Bhandari, J., Gelb, M. H., Brinker, A., Engels, I. H., Taylor, J., Chatterjee, A. K., … Kuhen, K. L. (2011). Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds. Molecular and Biochemical Parasitology, 175(1), 21-29. https://doi.org/10.1016/j.molbiopara.2010.08.005
Cui, L., Miao, J., & Cui, L. (2007). Cytotoxic effect of curcumin on malaria parasite Plasmodium falciparum: Inhibition of histone acetylation and generation of reactive oxygen species. Antimicrobial Agents and Chemotherapy, 51(2), 488-494. https://doi.org/10.1128/AAC.01238-06
Cui, L., Miao, J., Furuya, T., Fan, Q., Li, X., Rathod, P. K., Su, X.-Z., & Cui, L. (2008). Histone acetyltransferase inhibitor anacardic acid causes changes in global gene expression during in vitro Plasmodium falciparum development. Eukaryotic Cell, 7(7), 1200-1210. https://doi.org/10.1128/EC.00063-08
Cui, L., Miao, J., Furuya, T., Li, X., Su, X., & Cui, L. (2007). PfGCN5-mediated histone H3 acetylation plays a key role in gene expression in Plasmodium falciparum. Eukaryotic Cell, 6(7), 1219-1227. https://doi.org/10.1128/EC.00062-07
D'Alessandro, S., Silvestrini, F., Dechering, K., Corbett, Y., Parapini, S., Timmerman, M., Galastri, L., Basilico, N., Sauerwein, R., Alano, P., & Taramelli, D. (2013). A Plasmodium falciparum screening assay for anti-gametocyte drugs based on parasite lactate dehydrogenase detection. The Journal of Antimicrobial Chemotherapy, 68(9), 2048-2058. https://doi.org/10.1093/jac/dkt165
Darkin-Rattray, S. J., Gurnett, A. M., Myers, R. W., Dulski, P. M., Crumley, T. M., Allocco, J. J., Cannova, C., Meinke, P. T., Colletti, S. L., Bednarek, M. A., Singh, S. B., Goetz, M. A., Dombrowski, A. W., Polishook, J. D., & Schmatz, D. M. (1996). Apicidin: A novel antiprotozoal agent that inhibits parasite histone deacetylase. Proceedings of the National Academy of Sciences of the United States of America, 93(23), 13143-13147. https://doi.org/10.1073/pnas.93.23.13143
Delves, M., Lafuente-Monasterio, M. J., Upton, L., Ruecker, A., Leroy, D., Gamo, F.-J., & Sinden, R. (2019). Fueling open innovation for malaria transmission-blocking drugs: Hundreds of molecules targeting early parasite mosquito stages. Frontiers in Microbiology, 10, 2134. https://doi.org/10.3389/fmicb.2019.02134
Delves, M., Plouffe, D., Scheurer, C., Meister, S., Wittlin, S., Winzeler, E. A., Sinden, R. E., & Leroy, D. (2012). The activities of current antimalarial drugs on the life cycle stages of Plasmodium: A comparative study with human and rodent parasites. PLoS Medicine, 9(2), e1001169+. https://doi.org/10.1371/journal.pmed.1001169
Delves, M. J., Miguel-Blanco, C., Matthews, H., Molina, I., Ruecker, A., Yahiya, S., Straschil, U., Abraham, M., León, M. L., Fischer, O. J., Rueda-Zubiaurre, A., Brandt, J. R., Cortés, Á., Barnard, A., Fuchter, M. J., Calderón, F., Winzeler, E. A., Sinden, R. E., Herreros, E., … Baum, J. (2018). A high throughput screen for next-generation leads targeting malaria parasite transmission. Nature Communications, 9(1), 3805. https://doi.org/10.1038/s41467-018-05777-2
Delves, M. J., Straschil, U., Ruecker, A., Miguel-Blanco, C., Marques, S., Dufour, A. C., Baum, J., & Sinden, R. E. (2016). Routine in vitro culture of P. falciparum gametocytes to evaluate novel transmission-blocking interventions. Nature Protocols, 11(9), 1668-1680. https://doi.org/10.1038/nprot.2016.096
Demarta-Gatsi, C., Donini, C., Duffy, J., Sadler, C., Stewart, J., Barber, J. A., & Tornesi, B. (2022). Malarial PI4K inhibitor induced diaphragmatic hernias in rat: Potential link with mammalian kinase inhibition. Birth Defects Research, 114(10), 487-498. https://doi.org/10.1002/bdr2.2012
Derbyshire, E. R., Mazitschek, R., & Clardy, J. (2012). Characterization of Plasmodium liver stage inhibition by halofuginone. ChemMedChem, 7(5), 844-849. https://doi.org/10.1002/cmdc.201200045
Desai, S. A., Krogstad, D. J., & McCleskey, E. W. (1993). A nutrient-permeable channel on the intraerythrocytic malaria parasite. Nature, 362(6421), 643-646. https://doi.org/10.1038/362643a0
Dogovski, C., Xie, S. C., Burgio, G., Bridgford, J., Mok, S., McCaw, J. M., Chotivanich, K., Kenny, S., Gnädig, N., Straimer, J., Bozdech, Z., Fidock, D. A., Simpson, J. A., Dondorp, A. M., Foote, S., Klonis, N., & Tilley, L. (2015). Targeting the cell stress response of Plasmodium falciparum to overcome artemisinin resistance. PLoS Biology, 13(4), e1002132. https://doi.org/10.1371/journal.pbio.1002132
Dong, C. K., Urgaonkar, S., Cortese, J. F., Gamo, F.-J., Garcia-Bustos, J. F., Lafuente, M. J., Patel, V., Ross, L., Coleman, B. I., Derbyshire, E. R., Clish, C. B., Serrano, A. E., Cromwell, M., Barker, R. H., Dvorin, J. D., Duraisingh, M. T., Wirth, D. F., Clardy, J., & Mazitschek, R. (2011). Identification and validation of tetracyclic benzothiazepines as Plasmodium falciparum cytochrome bc1 inhibitors. Chemistry & Biology, 18(12), 1602-1610. https://doi.org/10.1016/j.chembiol.2011.09.016
Dorjsuren, D., Eastman, R. T., Wicht, K. J., Jansen, D., Talley, D. C., Sigmon, B. A., Zakharov, A. V., Roncal, N., Girvin, A. T., Antonova-Koch, Y., Will, P. M., Shah, P., Sun, H., Klumpp-Thomas, C., Mok, S., Yeo, T., Meister, S., Marugan, J. J., Ross, L. S., … Fidock, D. A. (2021). Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites. Scientific Reports, 11(1), 2121. https://doi.org/10.1038/s41598-021-81486-z
Douglas, R. G., Reinig, M., Neale, M., & Frischknecht, F. (2018). Screening for potential prophylactics targeting sporozoite motility through the skin. Malaria Journal, 17(1), 319. https://doi.org/10.1186/s12936-018-2469-0
Duffy, S., & Avery, V. M. (2013). Identification of inhibitors of Plasmodium falciparum gametocyte development. Malaria Journal, 12, 408. https://doi.org/10.1186/1475-2875-12-408
Dyer, M., Jackson, M., McWhinney, C., Zhao, G., & Mikkelsen, R. (1996). Analysis of a cation-transporting ATPase of Plasmodium falciparum. Molecular and Biochemical Parasitology, 78(1-2), 1-12. https://doi.org/10.1016/s0166-6851(96)02593-5
Eagon, S., Hammill, J. T., Sigal, M., Ahn, K. J., Tryhorn, J. E., Koch, G., Belanger, B., Chaplan, C. A., Loop, L., Kashtanova, A. S., Yniguez, K., Lazaro, H., Wilkinson, S. P., Rice, A. L., Falade, M. O., Takahashi, R., Kim, K., Cheung, A., DiBernardo, C., … Guy, R. K. (2020). Synthesis and structure-activity relationship of dual-stage antimalarial pyrazolo[3,4-b]pyridines. Journal of Medicinal Chemistry, 63(20), 11902-11919. https://doi.org/10.1021/acs.jmedchem.0c01152
El Bakkouri, M., Kouidmi, I., Wernimont, A. K., Amani, M., Hutchinson, A., Loppnau, P., Kim, J. J., Flueck, C., Walker, J. R., Seitova, A., Senisterra, G., Kakihara, Y., Kim, C., Blackman, M. J., Calmettes, C., Baker, D. A., & Hui, R. (2019). Structures of the cGMP-dependent protein kinase in malaria parasites reveal a unique structural relay mechanism for activation. Proceedings of the National Academy of Sciences of the United States of America, 116(28), 14164-14173. https://doi.org/10.1073/pnas.1905558116
Eldred, E. W., & Schimmel, P. R. (1972). Rapid deacylation by isoleucyl transfer ribonucleic acid synthetase of isoleucine-specific transfer ribonucleic acid aminoacylated with valine. The Journal of Biological Chemistry, 247(9), 2961-2964.
Fagbami, L., Deik, A. A., Singh, K., Santos, S. A., Herman, J. D., Bopp, S. E., Lukens, A. K., Clish, C. B., Wirth, D. F., & Mazitschek, R. (2019). The adaptive proline response in P. falciparum is independent of PfeIK1 and eIF2α signaling. ACS Infectious Diseases, 5(4), 515-520. https://doi.org/10.1021/acsinfecdis.8b00363
Fan, Q., An, L., & Cui, L. (2004). Plasmodium falciparum histone acetyltransferase, a yeast GCN5 homologue involved in chromatin remodeling. Eukaryotic Cell, 3(2), 264-276. https://doi.org/10.1128/EC.3.2.264-276.2004
Farooq, U., & Mahajan, R. C. (2004). Drug resistance in malaria. Journal of Vector Borne Diseases, 41(3-4), 45-53.
Fersht, A. R. (1977). Editing mechanisms in protein synthesis. Rejection of valine by the isoleucyl-tRNA synthetase. Biochemistry, 16(5), 1025-1030. https://doi.org/10.1021/bi00624a034
Fisher, N., Abd Majid, R., Antoine, T., Al-Helal, M., Warman, A. J., Johnson, D. J., Lawrenson, A. S., Ranson, H., O'Neill, P. M., Ward, S. A., & Biagini, G. A. (2012). Cytochrome b mutation Y268S conferring atovaquone resistance phenotype in malaria parasite results in reduced parasite bc1 catalytic turnover and protein expression. The Journal of Biological Chemistry, 287(13), 9731-9741. https://doi.org/10.1074/jbc.M111.324319
Fivelman, Q. L., Butcher, G. A., Adagu, I. S., Warhurst, D. C., & Pasvol, G. (2002). Malarone treatment failure and in vitro confirmation of resistance of Plasmodium falciparum isolate from Lagos, Nigeria. Malaria Journal, 1, 1. https://doi.org/10.1186/1475-2875-1-1
Forte, B., Ottilie, S., Plater, A., Campo, B., Dechering, K. J., Gamo, F. J., Goldberg, D. E., Istvan, E. S., Lee, M., Lukens, A. K., McNamara, C. W., Niles, J. C., Okombo, J., Pasaje, C. F. A., Siegel, M. G., Wirth, D., Wyllie, S., Fidock, D. A., Baragaña, B., … Gilbert, I. H. (2021). Prioritization of molecular targets for antimalarial drug discovery. ACS Infectious Diseases, 7(10), 2764-2776. https://doi.org/10.1021/acsinfecdis.1c00322
Fry, M., & Pudney, M. (1992). Site of action of the antimalarial hydroxynaphthoquinone, 2-[trans-4-(4′-chlorophenyl) cyclohexyl]-3-hydroxy-1,4-naphthoquinone (566C80). Biochemical Pharmacology, 43(7), 1545-1553. https://doi.org/10.1016/0006-2952(92)90213-3
Gambini, L., Rizzi, L., Pedretti, A., Taglialatela-Scafati, O., Carucci, M., Pancotti, A., Galli, C., Read, M., Giurisato, E., Romeo, S., & Russo, I. (2015). Picomolar inhibition of plasmepsin V, an essential malaria protease, achieved exploiting the prime region. PLoS ONE, 10(11), e0142509. https://doi.org/10.1371/journal.pone.0142509
Gantt, S. M., Myung, J. M., Briones, M. R., Li, W. D., Corey, E. J., Omura, S., Nussenzweig, V., & Sinnis, P. (1998). Proteasome inhibitors block development of Plasmodium spp. Antimicrobial Agents and Chemotherapy, 42(10), 2731-2738. https://doi.org/10.1128/AAC.42.10.2731
Gaur, A. H., McCarthy, J. S., Panetta, J. C., Dallas, R. H., Woodford, J., Tang, L., Smith, A. M., Stewart, T. B., Branum, K. C., Freeman, B. B., Patel, N. D., John, E., Chalon, S., Ost, S., Heine, R. N., Richardson, J. L., Christensen, R., Flynn, P. M., Van Gessel, Y., … Guy, R. K. (2020). Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: A first-in-human and induced blood-stage malaria phase 1a/b trial. The Lancet. Infectious Diseases, 20(8), 964-975. https://doi.org/10.1016/S1473-3099(19)30611-5
Giang, D. K., & Cravatt, B. F. (1998). A second mammalian N-myristoyltransferase. The Journal of Biological Chemistry, 273(12), 6595-6598. https://doi.org/10.1074/jbc.273.12.6595
Gillman, P. K. (2011). CNS toxicity involving methylene blue: The exemplar for understanding and predicting drug interactions that precipitate serotonin toxicity. Journal of Psychopharmacology (Oxford, England), 25(3), 429-436. https://doi.org/10.1177/0269881109359098
Gisselberg, J. E., Herrera, Z., Orchard, L. M., Llinás, M., & Yeh, E. (2018). Specific inhibition of the bifunctional farnesyl/geranylgeranyl diphosphate synthase in malaria parasites via a new small-molecule binding site. Cell Chemical Biology, 25(2), 185-193. http://view.ncbi.nlm.nih.gov/pubmed/29276048
Goncalves, V., Brannigan, J. A., Whalley, D., Ansell, K. H., Saxty, B., Holder, A. A., Wilkinson, A. J., Tate, E. W., & Leatherbarrow, R. J. (2012). Discovery of Plasmodium vivax N-myristoyltransferase inhibitors: Screening, synthesis, and structural characterization of their binding mode. Journal of Medicinal Chemistry, 55(7), 3578-3582. https://doi.org/10.1021/jm300040p
Goodman, C. D., Siregar, J. E., Mollard, V., Vega-Rodríguez, J., Syafruddin, D., Matsuoka, H., Matsuzaki, M., Toyama, T., Sturm, A., Cozijnsen, A., Jacobs-Lorena, M., Kita, K., Marzuki, S., & McFadden, G. I. (2016). Parasites resistant to the antimalarial atovaquone fail to transmit by mosquitoes. Science (New York, N.Y.), 352(6283), 349-353. https://doi.org/10.1126/science.aad9279
Graumans, W., Jacobs, E., Bousema, T., & Sinnis, P. (2020). When is a Plasmodium-infected mosquito an infectious mosquito? Trends in Parasitology, 36(8), 705-716. https://doi.org/10.1016/j.pt.2020.05.011
Hamerly, T., Tweedell, R. E., Hritzo, B., Nyasembe, V. O., Tekwani, B. L., Nanayakkara, N. P. D., Walker, L. A., & Dinglasan, R. R. (2019). NPC1161B, an 8-aminoquinoline analog, is metabolized in the mosquito and inhibits Plasmodium falciparum oocyst maturation. Frontiers in Pharmacology, 10, 1265. https://doi.org/10.3389/fphar.2019.01265
Harding, S. D., Armstrong, J. F., Faccenda, E., Southan, C., Alexander, S. P. H., Davenport, A. P., Pawson, A. J., Spedding, M., Davies, J. A., & NC-IUPHAR. (2021). The IUPHAR/BPS guide to PHARMACOLOGY in 2022: Curating pharmacology for COVID-19, malaria and antibacterials. Nucleic Acids Research, 50, D1282-D1294. https://doi.org/10.1093/nar/gkab1010
Hartuti, E. D., Sakura, T., Tagod, M. S. O., Yoshida, E., Wang, X., Mochizuki, K., Acharjee, R., Matsuo, Y., Tokumasu, F., Mori, M., Waluyo, D., Shiomi, K., Nozaki, T., Hamano, S., Shiba, T., Kita, K., & Inaoka, D. K. (2021). Identification of 3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives as novel selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. International Journal of Molecular Sciences, 22(13), 7236. https://doi.org/10.3390/ijms22137236
Harupa, A., De Las Heras, L., Colmenarejo, G., Lyons-Abbott, S., Reers, A., Caballero Hernandez, I., Chung, C.-W., Charter, D., Myler, P. J., Fernández-Menéndez, R. M., Calderón, F., Palomo, S., Rodríguez, B., Berlanga, M., Herreros-Avilés, E., Staker, B. L., Fernández Álvaro, E., & Kaushansky, A. (2020). Identification of selective inhibitors of Plasmodium N-myristoyltransferase by high-throughput screening. Journal of Medicinal Chemistry, 63(2), 591-600. https://doi.org/10.1021/acs.jmedchem.9b01343
Hassett, M. R., & Roepe, P. D. (2018). PIK-ing new malaria chemotherapy. Trends in Parasitology, 34(11), 925-927. https://doi.org/10.1016/j.pt.2018.06.003
Hayakawa, Y., Yamashita, T., Mori, T., Nagai, K., Shin-Ya, K., & Watanabe, H. (2004). Structure of tyroscherin, an antitumor antibiotic against IGF-1-dependent cells from Pseudallescheria sp. The Journal of Antibiotics, 57(10), 634-638. https://doi.org/10.7164/antibiotics.57.634
Heinemeyer, W., Fischer, M., Krimmer, T., Stachon, U., & Wolf, D. H. (1997). The active sites of the eukaryotic 20 S proteasome and their involvement in subunit precursor processing. The Journal of Biological Chemistry, 272(40), 25200-25209. https://doi.org/10.1074/jbc.272.40.25200
Hellmann, J. K., Münter, S., Wink, M., & Frischknecht, F. (2010). Synergistic and additive effects of epigallocatechin gallate and digitonin on Plasmodium sporozoite survival and motility. PLoS ONE, 5(1), e8682. https://doi.org/10.1371/journal.pone.0008682
Herman, J. D., Pepper, L. R., Cortese, J. F., Estiu, G., Galinsky, K., Zuzarte-Luis, V., Derbyshire, E. R., Ribacke, U., Lukens, A. K., Santos, S. A., Patel, V., Clish, C. B., Sullivan, W. J., Zhou, H., Bopp, S. E., Schimmel, P., Lindquist, S., Clardy, J., Mota, M. M., … Mazitschek, R. (2015). The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs. Science Translational Medicine, 7(288), 288ra77. https://doi.org/10.1126/scitranslmed.aaa3575
Herman, J. D., Rice, D. P., Ribacke, U., Silterra, J., Deik, A. A., Moss, E. L., Broadbent, K. M., Neafsey, D. E., Desai, M. M., Clish, C. B., Mazitschek, R., & Wirth, D. F. (2014). A genomic and evolutionary approach reveals non-genetic drug resistance in malaria. Genome Biology, 15(11), 511. https://doi.org/10.1186/PREACCEPT-1067113631444973
Hino, A., Hirai, M., Tanaka, T. Q., Watanabe, Y., Matsuoka, H., & Kita, K. (2012). Critical roles of the mitochondrial complex II in oocyst formation of rodent malaria parasite Plasmodium berghei. Journal of Biochemistry, 152(3), 259-268. https://doi.org/10.1093/jb/mvs058
Hodder, A. N., Sleebs, B. E., Czabotar, P. E., Gazdik, M., Xu, Y., O'Neill, M. T., Lopaticki, S., Nebl, T., Triglia, T., Smith, B. J., Lowes, K., Boddey, J. A., & Cowman, A. F. (2015). Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes. Nature Structural & Molecular Biology, 22(8), 590-596. https://doi.org/10.1038/nsmb.3061
Hoermann, A., Tapanelli, S., Capriotti, P., Del Corsano, G., Masters, E. K., Habtewold, T., Christophides, G. K., & Windbichler, N. (2021). Converting endogenous genes of the malaria mosquito into simple non-autonomous gene drives for population replacement. eLife, 10, e58791. https://doi.org/10.7554/eLife.58791
Hong, D. W., Leung, S. C., Amporndanai, K., Davies, J., Priestley, R. S., Nixon, G. L., Berry, N. G., Samar Hasnain, S., Antonyuk, S., Ward, S. A., Biagini, G. A., & O'Neill, P. M. (2018). Potent antimalarial 2-pyrazolyl quinolone bc 1 (Qi) inhibitors with improved drug-like properties. ACS Medicinal Chemistry Letters, 9(12), 1205-1210. https://doi.org/10.1021/acsmedchemlett.8b00371
Huang, J., Yuan, Y., Zhao, N., Pu, D., Tang, Q., Zhang, S., Luo, S., Yang, X., Wang, N., Xiao, Y., Zhang, T., Liu, Z., Sakata-Kato, T., Jiang, X., Kato, N., Yan, N., & Yin, H. (2021). Orthosteric-allosteric dual inhibitors of PfHT1 as selective antimalarial agents. Proceedings of the National Academy of Sciences of the United States of America, 118(3), e2017749118. https://doi.org/10.1073/pnas.2017749118
Huang, Z., Li, R., Tang, T., Ling, D., Wang, M., Xu, D., Sun, M., Zheng, L., Zhu, F., Min, H., Boonhok, R., Ding, Y., Wen, Y., Chen, Y., Li, X., Chen, Y., Liu, T., Han, J., Miao, J., … Jiang, L. (2020). A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1. Cell Discovery, 6(1), 93. https://doi.org/10.1038/s41421-020-00215-4
Hurdle, J. G., O'Neill, A. J., Ingham, E., Fishwick, C., & Chopra, I. (2004). Analysis of mupirocin resistance and fitness in Staphylococcus aureus by molecular genetic and structural modeling techniques. Antimicrobial Agents and Chemotherapy, 48(11), 4366-4376. https://doi.org/10.1128/AAC.48.11.4366-4376.2004
Hurt, D. E., Sutton, A. E., & Clardy, J. (2006). Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase. Bioorganic & Medicinal Chemistry Letters, 16(6), 1610-1615. https://doi.org/10.1016/j.bmcl.2005.12.029
Ibba, M., & Soll, D. (2000). Aminoacyl-tRNA synthesis. Annual Review of Biochemistry, 69, 617-650. https://doi.org/10.1146/annurev.biochem.69.1.617
Istvan, E. S., Dharia, N. V., Bopp, S. E., Gluzman, I., Winzeler, E. A., & Goldberg, D. E. (2011). Validation of isoleucine utilization targets in Plasmodium falciparum. Proceedings of the National Academy of Sciences of the United States of America, 108(4), 1627-1632. https://doi.org/10.1073/pnas.1011560108
Jain, V., Yogavel, M., Oshima, Y., Kikuchi, H., Touquet, B., Hakimi, M.-A., & Sharma, A. (2015). Structure of prolyl-tRNA synthetase-halofuginone complex provides basis for development of drugs against malaria and toxoplasmosis. Structure (London, England: 1993), 23(5), 819-829. https://doi.org/10.1016/j.str.2015.02.011
Jeffers, V., Gao, H., Checkley, L. A., Liu, Y., Ferdig, M. T., & Sullivan, W. J. (2016). Garcinol inhibits GCN5-mediated lysine acetyltransferase activity and prevents replication of the parasite Toxoplasma gondii. Antimicrobial Agents and Chemotherapy, 60(4), 2164-2170. https://doi.org/10.1128/AAC.03059-15
Jennison, C., Lucantoni, L., O'Neill, M. T., McConville, R., Erickson, S. M., Cowman, A. F., Sleebs, B. E., Avery, V. M., & Boddey, J. A. (2019). Inhibition of plasmepsin V activity blocks Plasmodium falciparum gametocytogenesis and transmission to mosquitoes. Cell Reports, 29(12), 3796-3806.e4. https://doi.org/10.1016/j.celrep.2019.11.073
Jiang, X., Yuan, Y., Huang, J., Zhang, S., Luo, S., Wang, N., Pu, D., Zhao, N., Tang, Q., Hirata, K., Yang, X., Jiao, Y., Sakata-Kato, T., Wu, J.-W., Yan, C., Kato, N., Yin, H., & Yan, N. (2020). Structural basis for blocking sugar uptake into the malaria parasite Plasmodium falciparum. Cell, 183(1), 258-268.e12. https://doi.org/10.1016/j.cell.2020.08.015
Jiménez-Díaz, M. B., Ebert, D., Salinas, Y., Pradhan, A., Lehane, A. M., Myrand-Lapierre, M.-E., O'Loughlin, K. G., Shackleford, D. M., Justino de Almeida, M., Carrillo, A. K., Clark, J. A., Dennis, A. S. M., Diep, J., Deng, X., Duffy, S., Endsley, A. N., Fedewa, G., Guiguemde, W. A., Gómez, M. G., … Guy, R. K. (2014). (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium. Proceedings of the National Academy of Sciences, 111(50), E5455-E5462. https://doi.org/10.1073/pnas.1414221111
Jordão, F. M., Gabriel, H. B., Alves, J. M. P., Angeli, C. B., Bifano, T. D., Breda, A., de Azevedo, M. F., Basso, L. A., Wunderlich, G., Kimura, E. A., & Katzin, A. M. (2013). Cloning and characterization of bifunctional enzyme farnesyl diphosphate/geranylgeranyl diphosphate synthase from Plasmodium falciparum. Malaria Journal, 12, 184. https://doi.org/10.1186/1475-2875-12-184
Jørgensen, R., Merrill, A. R., & Andersen, G. R. (2006). The life and death of translation elongation factor 2. Biochemical Society Transactions, 34(Pt 1), 1-6. https://doi.org/10.1042/BST20060001
Justice, M. C., Hsu, M. J., Tse, B., Ku, T., Balkovec, J., Schmatz, D., & Nielsen, J. (1998). Elongation factor 2 as a novel target for selective inhibition of fungal protein synthesis. The Journal of Biological Chemistry, 273(6), 3148-3151. https://doi.org/10.1074/jbc.273.6.3148
Kabeche, S., Aida, J., Akther, T., Ichikawa, T., Ochida, A., Pulkoski-Gross, M. J., Smith, M., Humphries, P. S., & Yeh, E. (2021). Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS. Bioorganic & Medicinal Chemistry Letters, 41, 127978. https://doi.org/10.1016/j.bmcl.2021.127978
Kandepedu, N., Gonzàlez Cabrera, D., Eedubilli, S., Taylor, D., Brunschwig, C., Gibhard, L., Njoroge, M., Lawrence, N., Paquet, T., Eyermann, C. J., Spangenberg, T., Basarab, G. S., Street, L. J., & Chibale, K. (2018). Identification, characterization, and optimization of 2,8-disubstituted-1,5-naphthyridines as novel Plasmodium falciparum phosphatidylinositol-4-kinase inhibitors with in vivo efficacy in a humanized mouse model of malaria. Journal of Medicinal Chemistry, 61(13), 5692-5703. https://doi.org/10.1021/acs.jmedchem.8b00648
Kanyal, A., Rawat, M., Gurung, P., Choubey, D., Anamika, K., & Karmodiya, K. (2018). Genome-wide survey and phylogenetic analysis of histone acetyltransferases and histone deacetylases of Plasmodium falciparum. The FEBS Journal, 285(10), 1767-1782. https://doi.org/10.1111/febs.14376
Kato, N., Comer, E., Sakata-Kato, T., Sharma, A., Sharma, M., Maetani, M., Bastien, J., Brancucci, N. M., Bittker, J. A., Corey, V., Clarke, D., Derbyshire, E. R., Dornan, G. L., Duffy, S., Eckley, S., Itoe, M. A., Koolen, K. M. J., Lewis, T. A., Lui, P. S., … Schreiber, S. L. (2016). Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature, 538(7625), 344-349. https://doi.org/10.1038/nature19804
Ke, H., Ganesan, S. M., Dass, S., Morrisey, J. M., Pou, S., Nilsen, A., Riscoe, M. K., Mather, M. W., & Vaidya, A. B. (2019). Mitochondrial type II NADH dehydrogenase of Plasmodium falciparum (PfNDH2) is dispensable in the asexual blood stages. PLoS ONE, 14(4), e0214023. https://doi.org/10.1371/journal.pone.0214023
Ke, H., Lewis, I. A., Morrisey, J. M., McLean, K. J., Ganesan, S. M., Painter, H. J., Mather, M. W., Jacobs-Lorena, M., Llinás, M., & Vaidya, A. B. (2015). Genetic investigation of tricarboxylic acid metabolism during the Plasmodium falciparum life cycle. Cell Reports, 11(1), 164-174. https://doi.org/10.1016/j.celrep.2015.03.011
Ke, H., Sigala, P. A., Miura, K., Morrisey, J. M., Mather, M. W., Crowley, J. R., Henderson, J. P., Goldberg, D. E., Long, C. A., & Vaidya, A. B. (2014). The heme biosynthesis pathway is essential for Plasmodium falciparum development in mosquito stage but not in blood stages. The Journal of Biological Chemistry, 289(50), 34827-34837. https://doi.org/10.1074/jbc.M114.615831
Kennedy, K., Cobbold, S. A., Hanssen, E., Birnbaum, J., Spillman, N. J., McHugh, E., Brown, H., Tilley, L., Spielmann, T., McConville, M. J., & Ralph, S. A. (2019). Delayed death in the malaria parasite Plasmodium falciparum is caused by disruption of prenylation-dependent intracellular trafficking. PLoS Biology, 17(7), e3000376. https://doi.org/10.1371/journal.pbio.3000376
Kheng, S., Muth, S., Taylor, W. R. J., Tops, N., Kosal, K., Sothea, K., Souy, P., Kim, S., Char, C. M., Vanna, C., Ly, P., Ringwald, P., Khieu, V., Kerleguer, A., Tor, P., Baird, J. K., Bjorge, S., Menard, D., & Christophel, E. (2015). Tolerability and safety of weekly primaquine against relapse of Plasmodium vivax in Cambodians with glucose-6-phosphate dehydrogenase deficiency. BMC Medicine, 13, 203. https://doi.org/10.1186/s12916-015-0441-1
Koehne, E., Kreidenweiss, A., Zoleko Manego, R., McCall, M., Mombo-Ngoma, G., Mackwitz, M. K. W., Hansen, F. K., & Held, J. (2019). Histone deacetylase inhibitors with high in vitro activities against Plasmodium falciparum isolates collected from Gabonese children and adults. Scientific Reports, 9(1), 17336. https://doi.org/10.1038/s41598-019-53912-w
Koh, C. Y., Kim, J. E., Napoli, A. J., Verlinde, C. L. M. J., Fan, E., Buckner, F. S., Van Voorhis, W. C., & Hol, W. G. J. (2013). Crystal structures of Plasmodium falciparum cytosolic tryptophanyl-tRNA synthetase and its potential as a target for structure-guided drug design. Molecular and Biochemical Parasitology, 189(1-2), 26-32. https://doi.org/10.1016/j.molbiopara.2013.04.007
Korsinczky, M., Chen, N., Kotecka, B., Saul, A., Rieckmann, K., & Cheng, Q. (2000). Mutations in Plasmodium falciparum cytochrome b that are associated with atovaquone resistance are located at a putative drug-binding site. Antimicrobial Agents and Chemotherapy, 44(8), 2100-2108. https://doi.org/10.1128/AAC.44.8.2100-2108.2000
Koussis, K., Withers-Martinez, C., Baker, D. A., & Blackman, M. J. (2020). Simultaneous multiple allelic replacement in the malaria parasite enables dissection of PKG function. Life Science Alliance, 3(4), e201900626. https://doi.org/10.26508/lsa.201900626
Krishnan, K., Ziniel, P., Li, H., Huang, X., Hupalo, D., Gombakomba, N., Guerrero, S. M., Dotrang, T., Lu, X., Caridha, D., Sternberg, A. R., Hughes, E., Sun, W., Bargieri, D. Y., Roepe, P. D., Sciotti, R. J., Wilkerson, M. D., Dalgard, C. L., Tawa, G. J., … Williamson, K. C. (2020). Torin 2 derivative, NCATS-SM3710, has potent multistage antimalarial activity through inhibition of P. falciparum phosphatidylinositol 4-kinase (Pf PI4KIIIβ). ACS Pharmacology & Translational Science, 3(5), 948-964. https://doi.org/10.1021/acsptsci.0c00078
Kuhen, K. L., Chatterjee, A. K., Rottmann, M., Gagaring, K., Borboa, R., Buenviaje, J., Chen, Z., Francek, C., Wu, T., Nagle, A., Barnes, S. W., Plouffe, D., Lee, M. C. S., Fidock, D. A., Graumans, W., Van De Vegte-Bolmer, M., Van Gemert, G. J., Wirjanata, G., Sebayang, B., … Diagana, T. T. (2014). KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrobial Agents and Chemotherapy, 58(9), 5060-5067. https://doi.org/10.1128/AAC.02727-13
Kumar, A., Bhowmick, K., Vikramdeo, K. S. S., Mondal, N., Subbarao, N., & Dhar, S. K. K. (2017). Designing novel inhibitors against histone acetyltransferase (HAT: GCN5) of Plasmodium falciparum. European Journal of Medicinal Chemistry, 138, 26-37.
LaMonte, G., Lim, M. Y.-X., Wree, M., Reimer, C., Nachon, M., Corey, V., Gedeck, P., Plouffe, D., Du, A., Figueroa, N., Yeung, B., Bifani, P., & Winzeler, E. A. (2016). Mutations in the Plasmodium falciparum cyclic amine resistance locus (PfCARL) confer multidrug resistance. MBio, 7(4), e00696-16. https://doi.org/10.1128/mBio.00696-16
LaMonte, G. M., Almaliti, J., Bibo-Verdugo, B., Keller, L., Zou, B. Y. Y., Yang, J., Antonova-Koch, Y., Orjuela-Sanchez, P., Boyle, C. A., Vigil, E., Wang, L., Goldgof, G. M., Gerwick, L., O'Donoghue, A. J., Winzeler, E. A., Gerwick, W. H., & Ottilie, S. (2017). Development of a potent inhibitor of the Plasmodium proteasome with reduced mammalian toxicity. Journal of Medicinal Chemistry, 60(15), 6721-6732.
Lane, K. D., Mu, J., Lu, J., Windle, S. T., Liu, A., Sun, P. D., & Wellems, T. E. (2018). Selection of Plasmodium falciparum cytochrome B mutants by putative PfNDH2 inhibitors. Proceedings of the National Academy of Sciences of the United States of America, 115(24), 6285-6290. https://doi.org/10.1073/pnas.1804492115
Laurens, M. B. (2020). RTS,S/AS01 vaccine (Mosquirix™): An overview. Human Vaccines & Immunotherapeutics, 16(3), 480-489. https://doi.org/10.1080/21645515.2019.1669415
Lehane, A. M., Ridgway, M. C., Baker, E., & Kirk, K. (2014). Diverse chemotypes disrupt ion homeostasis in the malaria parasite. Molecular Microbiology, 94(2), 327-339. https://doi.org/10.1111/mmi.12765
Li, H., O'Donoghue, A. J., van der Linden, W. A., Xie, S. C., Yoo, E., Foe, I. T., Tilley, L., Craik, C. S., da Fonseca, P. C., & Bogyo, M. (2016). Structure- and function-based design of Plasmodium-selective proteasome inhibitors. Nature, 530(7589), 233-236.
Li, R., Ling, D., Tang, T., Huang, Z., Wang, M., Ding, Y., Liu, T., Wei, H., Xu, W., Mao, F., Zhu, J., Li, X., Jiang, L., & Li, J. (2021). Discovery of novel Plasmodium falciparum HDAC1 inhibitors with dual-stage antimalarial potency and improved safety based on the clinical anticancer drug candidate quisinostat. Journal of Medicinal Chemistry, 64(4), 2254-2271. https://doi.org/10.1021/acs.jmedchem.0c02104
Liang, X., Jiang, Z., Huang, Z., Li, F., Chen, C., Hu, C., Wang, W., Hu, Z., Liu, Q., Wang, B., Wang, L., Qi, Z., Liu, J., Jiang, L., & Liu, Q. (2020). Discovery of 6′-chloro-N-methyl-5′-(phenylsulfonamido)-[3,3′-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium. European Journal of Medicinal Chemistry, 188, 112012. https://doi.org/10.1016/j.ejmech.2019.112012
Lim, M. Y.-X. Y., LaMonte, G., Lee, M. C., Reimer, C., Tan, B. H. H., Corey, V., Tjahjadi, B. F., Chua, A., Nachon, M., Wintjens, R., Gedeck, P., Malleret, B., Renia, L., Bonamy, G. M., Ho, P. C.-L. C., Yeung, B. K., Chow, E. D., Lim, L., Fidock, D. A., … Bifani, P. (2016). UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes. Nature Microbiology, 1, 16166. https://doi.org/10.1038/nmicrobiol.2016.166 http://view.ncbi.nlm.nih.gov/pubmed/27642791
Liu, S., Neidhardt, E. A., Grossman, T. H., Ocain, T., & Clardy, J. (2000). Structures of human dihydroorotate dehydrogenase in complex with antiproliferative agents. Structure (London, England: 1993), 8(1), 25-33. https://doi.org/10.1016/s0969-2126(00)00077-0
Llanos-Cuentas, A., Casapia, M., Chuquiyauri, R., Hinojosa, J.-C. C., Kerr, N., Rosario, M., Toovey, S., Arch, R. H., Phillips, M. A., Rozenberg, F. D., Bath, J., Ng, C. L., Cowell, A. N., Winzeler, E. A., Fidock, D. A., Baker, M., Möhrle, J. J., Hooft van Huijsduijnen, R., Gobeau, N., … Duparc, S. (2018). Antimalarial activity of single-dose DSM265, a novel Plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: A proof-of-concept, open-label, phase 2a study. The Lancet. Infectious Diseases. http://view.ncbi.nlm.nih.gov/pubmed/29909069, 18, 874-883. https://doi.org/10.1016/S1473-3099(18)30309-8
Looareesuwan, S., Viravan, C., Webster, H. K., Kyle, D. E., Hutchinson, D. B., & Canfield, C. J. (1996). Clinical studies of atovaquone, alone or in combination with other antimalarial drugs, for treatment of acute uncomplicated malaria in Thailand. The American Journal of Tropical Medicine and Hygiene, 54(1), 62-66. https://doi.org/10.4269/ajtmh.1996.54.62
Lucantoni, L., Duffy, S., Adjalley, S. H., Fidock, D. A., & Avery, V. M. (2013). Identification of MMV malaria box inhibitors of Plasmodium falciparum early-stage gametocytes using a luciferase-based high-throughput assay. Antimicrobial Agents and Chemotherapy, 57(12), 6050-6062. https://doi.org/10.1128/AAC.00870-13
Luth, M. R., Gupta, P., Ottilie, S., & Winzeler, E. A. (2018). Using in vitro evolution and whole genome analysis to discover next generation targets for antimalarial drug discovery. ACS Infectious Diseases, 4(3), 301-314. https://doi.org/10.1021/acsinfecdis.7b00276
MacRae, J. I., Dixon, M. W., Dearnley, M. K., Chua, H. H., Chambers, J. M., Kenny, S., Bottova, I., Tilley, L., & McConville, M. J. (2013). Mitochondrial metabolism of sexual and asexual blood stages of the malaria parasite Plasmodium falciparum. BMC Biology, 11, 67. https://doi.org/10.1186/1741-7007-11-67
Maetani, M., Kato, N., Jabor, V. A. P., Calil, F. A., Nonato, M. C., Scherer, C. A., & Schreiber, S. L. (2017). Discovery of antimalarial azetidine-2-carbonitriles that inhibit P. falciparum dihydroorotate dehydrogenase. ACS Medicinal Chemistry Letters, 8(4), 438-442. https://doi.org/10.1021/acsmedchemlett.7b00030
Magistrado, P. A., Corey, V. C., Lukens, A. K., LaMonte, G., Sasaki, E., Meister, S., Wree, M., Winzeler, E., & Wirth, D. F. (2016). Plasmodium falciparum cyclic amine resistance locus (PfCARL), a resistance mechanism for two distinct compound classes. ACS Infectious Diseases, 2(11), 816-826. https://doi.org/10.1021/acsinfecdis.6b00025
Mahindra, A., Janha, O., Mapesa, K., Sanchez-Azqueta, A., Alam, M. M., Amambua-Ngwa, A., Nwakanma, D. C., Tobin, A. B., & Jamieson, A. G. (2020). Development of potent PfCLK3 inhibitors based on TCMDC-135051 as a new class of antimalarials. Journal of Medicinal Chemistry, 63(17), 9300-9315. https://doi.org/10.1021/acs.jmedchem.0c00451
Maier, A. G., Cooke, B. M., Cowman, A. F., & Tilley, L. (2009). Malaria parasite proteins that remodel the host erythrocyte. Nature Reviews. Microbiology, 7(5), 341-354. https://doi.org/10.1038/nrmicro2110
Maier, A. G., Rug, M., O'Neill, M. T., Brown, M., Chakravorty, S., Szestak, T., Chesson, J., Wu, Y., Hughes, K., Coppel, R. L., Newbold, C., Beeson, J. G., Craig, A., Crabb, B. S., & Cowman, A. F. (2008). Exported proteins required for virulence and rigidity of Plasmodium falciparum-infected human erythrocytes. Cell, 134(1), 48-61. https://doi.org/10.1016/j.cell.2008.04.051
Mairet-Khedim, M., Leang, R., Marmai, C., Khim, N., Kim, S., Ke, S., Kauy, C., Kloeung, N., Eam, R., Chy, S., Izac, B., Mey Bouth, D., Dorina Bustos, M., Ringwald, P., Ariey, F., & Witkowski, B. (2020). Clinical and in vitro resistance of Plasmodium falciparum to artesunate-amodiaquine in Cambodia. Clinical Infectious Diseases, 73, 406-413. https://doi.org/10.1093/cid/ciaa628
Maka, D. E., Chiabi, A., Ndikum, V., Achu, D., Mah, E., Nguefack, S., Nana, P., Njoumemi, Z., Mbacham, W., & Mbonda, E. (2015). A randomized trial of the efficacy of artesunate and three quinine regimens in the treatment of severe malaria in children at the Ebolowa Regional Hospital, Cameroon. Malaria Journal, 14, 429. https://doi.org/10.1186/s12936-015-0948-0
Mandt, R. E. K., Lafuente-Monasterio, M. J., Sakata-Kato, T., Luth, M. R., Segura, D., Pablos-Tanarro, A., Viera, S., Magan, N., Ottilie, S., Winzeler, E. A., Lukens, A. K., Gamo, F. J., & Wirth, D. F. (2019). In vitro selection predicts malaria parasite resistance to dihydroorotate dehydrogenase inhibitors in a mouse infection model. Science Translational Medicine, 11(521), eaav1636. https://doi.org/10.1126/scitranslmed.aav1636
Manickam, Y., Chaturvedi, R., Babbar, P., Malhotra, N., Jain, V., & Sharma, A. (2018). Drug targeting of one or more aminoacyl-tRNA synthetase in the malaria parasite Plasmodium falciparum. Drug Discovery Today, 23(6), 1233-1240. https://doi.org/10.1016/j.drudis.2018.01.050
Marfurt, J., Chalfein, F., Prayoga, P., Wabiser, F., Kenangalem, E., Piera, K. A., Fairlie, D. P., Tjitra, E., Anstey, N. M., Andrews, K. T., & Price, R. N. (2011). Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. Antimicrobial Agents and Chemotherapy, 55(3), 961-966. https://doi.org/10.1128/AAC.01220-10
Matralis, A. N., Malik, A., Penzo, M., Moreno, I., Almela, M. J., Camino, I., Crespo, B., Saadeddin, A., Ghidelli-Disse, S., Rueda, L., Calderon, F., Osborne, S. A., Drewes, G., Böesche, M., Fernández-Álvaro, E., Martin Hernando, J. I., & Baker, D. A. (2019). Development of chemical entities endowed with potent fast-killing properties against Plasmodium falciparum malaria parasites. Journal of Medicinal Chemistry, 62(20), 9217-9235. https://doi.org/10.1021/acs.jmedchem.9b01099
Matteucci, K. C., Correa, A. A. S., & Costa, D. L. (2022). Recent advances in host-directed therapies for tuberculosis and malaria. Frontiers in Cellular and Infection Microbiology, 12, 905278. https://doi.org/10.3389/fcimb.2022.905278
Mbugi, E. V., Mutayoba, B. M., Malisa, A. L., Balthazary, S. T., Nyambo, T. B., & Mshinda, H. (2006). Drug resistance to sulphadoxine-pyrimethamine in Plasmodium falciparum malaria in Mlimba, Tanzania. Malaria Journal, 5, 94. https://doi.org/10.1186/1475-2875-5-94
McCarthy, J. S., Donini, C., Chalon, S., Woodford, J., Marquart, L., Collins, K. A., Rozenberg, F. D., Fidock, D. A., Cherkaoui-Rbati, M. H., Gobeau, N., & Möhrle, J. J. (2020). A phase 1, placebo-controlled, randomized, single ascending dose study and a volunteer infection study to characterize the safety, pharmacokinetics, and antimalarial activity of the Plasmodium phosphatidylinositol 4-kinase inhibitor MMV390048. Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America, 71(10), e657-e664. https://doi.org/10.1093/cid/ciaa368
McNamara, C. W., Lee, M. C., Lim, C. S. S., Lim, S. H. H., Roland, J., Nagle, A., Simon, O., Yeung, B. K., Chatterjee, A. K., McCormack, S. L., Manary, M. J., Zeeman, A.-M. M., Dechering, K. J., Kumar, S. R., Henrich, P. P., Gagaring, K., Ibanez, M., Kato, N., Kuhen, K. L., … Winzeler, E. A. (2013). Targeting Plasmodium PI(4)K to eliminate malaria. Nature, 504(7479), 248-253. https://doi.org/10.1038/nature12782
McRobert, L., Taylor, C. J., Deng, W., Fivelman, Q. L., Cummings, R. M., Polley, S. D., Billker, O., & Baker, D. A. (2008). Gametogenesis in malaria parasites is mediated by the cGMP-dependent protein kinase. PLoS Biology, 6(6), e139. https://doi.org/10.1371/journal.pbio.0060139
Meister, S., Plouffe, D. M., Kuhen, K. L., Bonamy, G. M., Wu, T., Barnes, S. W., Bopp, S. E., Borboa, R., Bright, A. T., Che, J., Cohen, S., Dharia, N. V., Gagaring, K., Gettayacamin, M., Gordon, P., Groessl, T., Kato, N., Lee, M. C., McNamara, C. W., … Winzeler, E. A. (2011). Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science (New York, N.Y.), 334(6061), 1372-1377. https://doi.org/10.1126/science.1211936
Meshnick, S. R., & Dobson, M. J. (2001). The history of antimalarial drugs. In P. J. Rosenthal (Ed.), Antimalarial chemotherapy. Infectious disease. Antimalarial Chemotherapy. Humana Press.
Miao, J., Wang, C., Lucky, A. B., Liang, X., Min, H., Adapa, S. R., Jiang, R., Kim, K., & Cui, L. (2021). A unique GCN5 histone acetyltransferase complex controls erythrocyte invasion and virulence in the malaria parasite Plasmodium falciparum. PLoS Pathogens, 17(8), e1009351. https://doi.org/10.1371/journal.ppat.1009351
Miranda-Saavedra, D., Gabaldón, T., Barton, G. J., Langsley, G., & Doerig, C. (2012). The kinomes of apicomplexan parasites. Microbes and Infection, 14(10), 796-810. https://doi.org/10.1016/j.micinf.2012.04.007
Mohammed, R., Asres, M. S., Gudina, E. K., Adissu, W., Johnstone, H., Marrast, A. C., Donini, C., Duparc, S., & Yilma, D. (2023). Efficacy, safety, tolerability, and pharmacokinetics of MMV390048 in acute uncomplicated malaria. The American Journal of Tropical Medicine and Hygiene, 108(1), 81-84. https://doi.org/10.4269/ajtmh.22-0567
Mott, B. T., Eastman, R. T., Guha, R., Sherlach, K. S., Siriwardana, A., Shinn, P., McKnight, C., Michael, S., Lacerda-Queiroz, N., Patel, P. R., Khine, P., Sun, H., Kasbekar, M., Aghdam, N., Fontaine, S. D., Liu, D., Mierzwa, T., Mathews-Griner, L. A., Ferrer, M., … Thomas, C. J. (2015). High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations. Scientific Reports, 5, 13891. https://doi.org/10.1038/srep13891
Moustakim, M., Clark, P. G. K., Trulli, L., Fuentes de Arriba, A. L., Ehebauer, M. T., Chaikuad, A., Murphy, E. J., Mendez-Johnson, J., Daniels, D., Hou, C.-F. D., Lin, Y.-H., Walker, J. R., Hui, R., Yang, H., Dorrell, L., Rogers, C. M., Monteiro, O. P., Fedorov, O., Huber, K. V. M., … Brennan, P. E. (2017). Discovery of a PCAF bromodomain chemical probe. Angewandte Chemie (International Ed. in English), 56(3), 827-831. https://doi.org/10.1002/anie.201610816
Munro, B. A., & McMorran, B. J. (2022). Antimalarial drug strategies to target Plasmodium gametocytes. Parasitologia, 2(2), 101-124. https://doi.org/10.3390/parasitologia2020011
Nagaraj, V. A., Sundaram, B., Varadarajan, N. M., Subramani, P. A., Kalappa, D. M., Ghosh, S. K., & Padmanaban, G. (2013). Malaria parasite-synthesized heme is essential in the mosquito and liver stages and complements host heme in the blood stages of infection. PLoS Pathogens, 9(8), e1003522. https://doi.org/10.1371/journal.ppat.1003522
Nam, T.-G., McNamara, C. W., Bopp, S., Dharia, N. V., Meister, S., Bonamy, G. M. C., Plouffe, D. M., Kato, N., McCormack, S., Bursulaya, B., Ke, H., Vaidya, A. B., Schultz, P. G., & Winzeler, E. A. (2011). A chemical genomic analysis of decoquinate, a Plasmodium falciparum cytochrome b inhibitor. ACS Chemical Biology, 6(11), 1214-1222. https://doi.org/10.1021/cb200105d
Ndayisaba, G., Yeka, A., Asante, K. P., Grobusch, M. P., Karita, E., Mugerwa, H., Asiimwe, S., Oduro, A., Fofana, B., Doumbia, S., Jain, J. P., Barsainya, S., Kullak-Ublick, G. A., Su, G., Schmitt, E. K., Csermak, K., Gandhi, P., & Hughes, D. (2021). Hepatic safety and tolerability of cipargamin (KAE609), in adult patients with Plasmodium falciparum malaria: A randomized, phase II, controlled, dose-escalation trial in sub-Saharan Africa. Malaria Journal, 20(1), 478. https://doi.org/10.1186/s12936-021-04009-1
Nilsen, A., LaCrue, A. N., White, K. L., Forquer, I. P., Cross, R. M., Marfurt, J., Mather, M. W., Delves, M. J., Shackleford, D. M., Saenz, F. E., Morrisey, J. M., Steuten, J., Mutka, T., Li, Y., Wirjanata, G., Ryan, E., Duffy, S., Kelly, J. X., Sebayang, B. F., … Riscoe, M. K. (2013). Quinolone-3-diarylethers: A new class of antimalarial drug. Science Translational Medicine, 5(177), 177ra37. https://doi.org/10.1126/scitranslmed.3005029
Nilsen, A., Miley, G. P., Forquer, I. P., Mather, M. W., Katneni, K., Li, Y., Pou, S., Pershing, A. M., Stickles, A. M., Ryan, E., Kelly, J. X., Doggett, J. S., White, K. L., Hinrichs, D. J., Winter, R. W., Charman, S. A., Zakharov, L. N., Bathurst, I., Burrows, J. N., … Riscoe, M. K. (2014). Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers. Journal of Medicinal Chemistry, 57(9), 3818-3834. https://doi.org/10.1021/jm500147k
No, J. H., de Dossin, F. M., Zhang, Y., Liu, Y.-L., Zhu, W., Feng, X., Yoo, J. A., Lee, E., Wang, K., Hui, R., Freitas-Junior, L. H., & Oldfield, E. (2012). Lipophilic analogs of zoledronate and risedronate inhibit Plasmodium geranylgeranyl diphosphate synthase (GGPPS) and exhibit potent antimalarial activity. Proceedings of the National Academy of Sciences, 109(11), 4058-4063. https://doi.org/10.1073/pnas.1118215109
Nyamai, D. W., & Tastan Bishop, Ö. (2019). Aminoacyl tRNA synthetases as malarial drug targets: A comparative bioinformatics study. Malaria Journal, 18(1), 34. https://doi.org/10.1186/s12936-019-2665-6
Nzila, A. (2006). The past, present and future of antifolates in the treatment of Plasmodium falciparum infection. The Journal of Antimicrobial Chemotherapy, 57(6), 1043-1054. https://doi.org/10.1093/jac/dkl104
Okaniwa, M., Shibata, A., Ochida, A., Akao, Y., White, K. L., Shackleford, D. M., Duffy, S., Lucantoni, L., Dey, S., Striepen, J., Yeo, T., Mok, S., Aguiar, A. C. C., Sturm, A., Crespo, B., Sanz, L. M., Churchyard, A., Baum, J., Pereira, D. B., … Laleu, B. (2021). Repositioning and characterization of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives as Plasmodium cytoplasmic prolyl-tRNA synthetase inhibitors. ACS Infectious Diseases, 7(6), 1680-1689. https://doi.org/10.1021/acsinfecdis.1c00020
Onoabedje, E. A., Ibezim, A., Okoro, U. C., & Batra, S. (2021). New sulphonamide pyrolidine carboxamide derivatives: Synthesis, molecular docking, antiplasmodial and antioxidant activities. PLoS ONE, 16(2), e0243305. https://doi.org/10.1371/journal.pone.0243305
Orlowski, R. Z., Stinchcombe, T. E., Mitchell, B. S., Shea, T. C., Baldwin, A. S., Stahl, S., Adams, J., Esseltine, D.-L., Elliott, P. J., Pien, C. S., Guerciolini, R., Anderson, J. K., Depcik-Smith, N. D., Bhagat, R., Lehman, M. J., Novick, S. C., O'Connor, O. A., & Soignet, S. L. (2002). Phase I trial of the proteasome inhibitor PS-341 in patients with refractory hematologic malignancies. Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology, 20(22), 4420-4427. https://doi.org/10.1200/JCO.2002.01.133
Painter, H. J., Morrisey, J. M., Mather, M. W., & Vaidya, A. B. (2007). Specific role of mitochondrial electron transport in blood-stage Plasmodium falciparum. Nature, 446(7131), 88-91. https://doi.org/10.1038/nature05572
Palencia, A., Bougdour, A., Brenier-Pinchart, M.-P., Touquet, B., Bertini, R.-L., Sensi, C., Gay, G., Vollaire, J., Josserand, V., Easom, E., Freund, Y. R., Pelloux, H., Rosenthal, P. J., Cusack, S., & Hakimi, M.-A. (2017). Targeting Toxoplasma gondii CPSF3 as a new approach to control toxoplasmosis. EMBO Molecular Medicine, 9(3), 385-394. https://doi.org/10.15252/emmm.201607370
Paquet, T., Le Manach, C., Cabrera, D. G., Younis, Y., Henrich, P. P., Abraham, T. S., Lee, M. C. S., Basak, R., Ghidelli-Disse, S., Lafuente-Monasterio, M. J., Bantscheff, M., Ruecker, A., Blagborough, A. M., Zakutansky, S. E., Zeeman, A.-M., White, K. L., Shackleford, D. M., Mannila, J., Morizzi, J., … Chibale, K. (2017). Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase. Science Translational Medicine, 9(387), eaad9735. https://doi.org/10.1126/scitranslmed.aad9735
Pasaje, C. F. A., Cheung, V., Kennedy, K., Lim, E. E., Baell, J. B., Griffin, M. D. W., & Ralph, S. A. (2016). Selective inhibition of apicoplast tryptophanyl-tRNA synthetase causes delayed death in Plasmodium falciparum. Scientific Reports, 6, 27531. https://doi.org/10.1038/srep27531
Paton, D. G., Childs, L. M., Itoe, M. A., Holmdahl, I. E., Buckee, C. O., & Catteruccia, F. (2019). Exposing Anopheles mosquitoes to antimalarials blocks Plasmodium parasite transmission. Nature, 567(7747), 239-243. https://doi.org/10.1038/s41586-019-0973-1
Penzo, M., de Las Heras-Dueña, L., Mata-Cantero, L., Diaz-Hernandez, B., Vazquez-Muñiz, M.-J., Ghidelli-Disse, S., Drewes, G., Fernandez-Alvaro, E., & Baker, D. A. (2019). High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage parasites. Scientific Reports, 9(1), 7005. https://doi.org/10.1038/s41598-019-42801-x
Peterson, D. S., Milhous, W. K., & Wellems, T. E. (1990). Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria. Proceedings of the National Academy of Sciences of the United States of America, 87(8), 3018-3022. https://doi.org/10.1073/pnas.87.8.3018
Phillips, M. A., Lotharius, J., Marsh, K., White, J., Dayan, A., White, K. L., Njoroge, J. W., Mazouni, F. E., Lao, Y., Kokkonda, S., Tomchick, D. R., Deng, X., Laird, T., Bhatia, S. N., March, S., Ng, C. L., Fidock, D. A., Wittlin, S., Lafuente-Monasterio, M., … Charman, S. A. (2015). A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Science Translational Medicine, 7(296), 296ra111. https://doi.org/10.1126/scitranslmed.aaa6645
Plouffe, D. M., Wree, M., Du, A. Y., Meister, S., Li, F., Patra, K., Lubar, A., Okitsu, S. L., Flannery, E. L., Kato, N., Tanaseichuk, O., Comer, E., Zhou, B., Kuhen, K., Zhou, Y., Leroy, D., Schreiber, S. L., Scherer, C. A., Vinetz, J., & Winzeler, E. A. (2016). High-throughput assay and discovery of small molecules that interrupt malaria transmission. Cell Host & Microbe, 19(1), 114-126. https://doi.org/10.1016/j.chom.2015.12.001
Polino, A. J., Nasamu, A. S., Niles, J. C., & Goldberg, D. E. (2020). Assessment of biological role and insight into druggability of the Plasmodium falciparum protease plasmepsin V. ACS Infectious Diseases, 6(4), 738-746. https://doi.org/10.1021/acsinfecdis.9b00460
Poonam, Gupta, Y., Gupta, N., Singh, S., Wu, L., Chhikara, B. S., Rawat, M., & Rathi, B. (2018). Multistage inhibitors of the malaria parasite: Emerging hope for chemoprotection and malaria eradication. Medicinal Research Reviews, 38, 1511-1535. https://doi.org/10.1002/med.21486
Posayapisit, N., Pengon, J., Prommana, P., Shoram, M., Yuthavong, Y., Uthaipibull, C., Kamchonwongpaisan, S., & Jupatanakul, N. (2021). Transgenic pyrimethamine-resistant Plasmodium falciparum reveals transmission-blocking potency of P218, a novel antifolate candidate drug. International Journal for Parasitology, 51(8), 635-642. https://doi.org/10.1016/j.ijpara.2020.12.002
Potluri, V., Shandil, R. K., Gavara, R., Sambasivam, G., Campo, B., Wittlin, S., & Narayanan, S. (2020). Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malaria Journal, 19(1), 365. https://doi.org/10.1186/s12936-020-03421-3
Qureshi, A. A., Suades, A., Matsuoka, R., Brock, J., McComas, S. E., Nji, E., Orellana, L., Claesson, M., Delemotte, L., & Drew, D. (2020). The molecular basis for sugar import in malaria parasites. Nature, 578(7794), 321-325. https://doi.org/10.1038/s41586-020-1963-z
Rackham, M. D., Brannigan, J. A., Moss, D. K., Yu, Z., Wilkinson, A. J., Holder, A. A., Tate, E. W., & Leatherbarrow, R. J. (2013). Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase. Journal of Medicinal Chemistry, 56(1), 371-375. https://doi.org/10.1021/jm301474t
Ranson, H., N'guessan, R., Lines, J., Moiroux, N., Nkuni, Z., & Corbel, V. (2011). Pyrethroid resistance in African anopheline mosquitoes: What are the implications for malaria control? Trends in Parasitology, 27(2), 91-98. https://doi.org/10.1016/j.pt.2010.08.004
Rawat, M., Kanyal, A., Sahasrabudhe, A., Vembar, S. S., Lopez-Rubio, J.-J., & Karmodiya, K. (2021). Histone acetyltransferase PfGCN5 regulates stress responsive and artemisinin resistance related genes in Plasmodium falciparum. Scientific Reports, 11(1), 852. https://doi.org/10.1038/s41598-020-79539-w
Reader, J., van der Watt, M. E., Taylor, D., Le Manach, C., Mittal, N., Ottilie, S., Theron, A., Moyo, P., Erlank, E., Nardini, L., Venter, N., Lauterbach, S., Bezuidenhout, B., Horatscheck, A., van Heerden, A., Spillman, N. J., Cowell, A. N., Connacher, J., Opperman, D., … Birkholtz, L.-M. (2021). Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box. Nature Communications, 12(1), 269. https://doi.org/10.1038/s41467-020-20629-8
Reynolds, J. M., El Bissati, K., Brandenburg, J., Günzl, A., & Mamoun, C. B. (2007). Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL3B. BMC Clinical Pharmacology, 7, 13. https://doi.org/10.1186/1472-6904-7-13
Rieckmann, K. H., Yeo, A. E., & Edstein, M. D. (1996). Activity of PS-15 and its metabolite, WR99210, against Plasmodium falciparum in an in vivo-in vitro model. Transactions of the Royal Society of Tropical Medicine and Hygiene, 90(5), 568-571. https://doi.org/10.1016/s0035-9203(96)90326-0
Ro, D.-K., Paradise, E. M., Ouellet, M., Fisher, K. J., Newman, K. L., Ndungu, J. M., Ho, K. A., Eachus, R. A., Ham, T. S., Kirby, J., Chang, M. C. Y., Withers, S. T., Shiba, Y., Sarpong, R., & Keasling, J. D. (2006). Production of the antimalarial drug precursor artemisinic acid in engineered yeast. Nature, 440(7086), 940-943. https://doi.org/10.1038/nature04640
Roskoski, R. (2020). Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update. Pharmacological Research, 152, 104609. https://doi.org/10.1016/j.phrs.2019.104609
Ross, L. S., Gamo, F. J., Lafuente-Monasterio, M. J., Singh, O. M. P., Rowland, P., Wiegand, R. C., & Wirth, D. F. (2014). In vitro resistance selections for Plasmodium falciparum dihydroorotate dehydrogenase inhibitors give mutants with multiple point mutations in the drug-binding site and altered growth. The Journal of Biological Chemistry, 289(26), 17980-17995. https://doi.org/10.1074/jbc.M114.558353
Rottmann, M., McNamara, C., Yeung, B. K. S., Lee, M. C. S., Zou, B., Russell, B., Seitz, P., Plouffe, D. M., Dharia, N. V., Tan, J., Cohen, S. B., Spencer, K. R., González-Páez, G. E., Lakshminarayana, S. B., Goh, A., Suwanarusk, R., Jegla, T., Schmitt, E. K., Beck, H.-P., … Diagana, T. T. (2010). Spiroindolones, a potent compound class for the treatment of malaria. Science, 329(5996), 1175-1180. https://doi.org/10.1126/science.1193225
Ruecker, A., Mathias, D. K., Straschil, U., Churcher, T. S., Dinglasan, R. R., Leroy, D., Sinden, R. E., & Delves, M. J. (2014). A male and female gametocyte functional viability assay to identify biologically relevant malaria transmission-blocking drugs. Antimicrobial Agents and Chemotherapy, 58(12), 7292-7302. https://doi.org/10.1128/AAC.03666-14
Russo, I., Babbitt, S., Muralidharan, V., Butler, T., Oksman, A., & Goldberg, D. E. (2010). Plasmepsin V licenses Plasmodium proteins for export into the host erythrocyte. Nature, 463(7281), 632-636. https://doi.org/10.1038/nature08726
Saliba, K. J., & Kirk, K. (1999). pH regulation in the intracellular malaria parasite, Plasmodium falciparum. H(+) extrusion via a V-type H(+)-ATPase. The Journal of Biological Chemistry, 274(47), 33213-33219. https://doi.org/10.1074/jbc.274.47.33213
Sanders, N. G., Sullivan, D. J., Mlambo, G., Dimopoulos, G., & Tripathi, A. K. (2014). Gametocytocidal screen identifies novel chemical classes with Plasmodium falciparum transmission blocking activity. PLoS ONE, 9(8), e105817. https://doi.org/10.1371/journal.pone.0105817
Schlitzer, M. (2007). Malaria chemotherapeutics part I: History of antimalarial drug development, currently used therapeutics, and drugs in clinical development. ChemMedChem, 2(7), 944-986. https://doi.org/10.1002/cmdc.200600240
Schlott, A. C., Holder, A. A., & Tate, E. W. (2018). N-Myristoylation as a drug target in malaria: Exploring the role of N-myristoyltransferase substrates in the inhibitor mode of action. ACS Infectious Diseases, 4(4), 449-457.
Schlott, A. C., Mayclin, S., Reers, A. R., Coburn-Flynn, O., Bell, A. S., Green, J., Knuepfer, E., Charter, D., Bonnert, R., Campo, B., Burrows, J., Lyons-Abbott, S., Staker, B. L., Chung, C.-W., Myler, P. J., Fidock, D. A., Tate, E. W., & Holder, A. A. (2019). Structure-guided identification of resistance breaking antimalarial N-myristoyltransferase inhibitors. Cell Chemical Biology, 26(7), 991-1000.e7. https://doi.org/10.1016/j.chembiol.2019.03.015
Shastry, M., Nielsen, J., Ku, T., Hsu, M.-J., Liberator, P., Anderson, J., Schmatz, D., & Justice, M. C. (2001). Species-specific inhibition of fungal protein synthesis by sordarin: Identification of a sordarin-specificity region in eukaryotic elongation factor 2. Microbiology (Reading, England), 147(Pt 2), 383-390. https://doi.org/10.1099/00221287-147-2-383
Shibata, A., Kuno, M., Adachi, R., Sato, Y., Hattori, H., Matsuda, A., Okuzono, Y., Igaki, K., Tominari, Y., Takagi, T., Yabuki, M., & Okaniwa, M. (2017). Discovery and pharmacological characterization of a new class of prolyl-tRNA synthetase inhibitor for anti-fibrosis therapy. PLoS ONE, 12(10), e0186587. https://doi.org/10.1371/journal.pone.0186587
Sicard, A., Semblat, J.-P., Doerig, C., Hamelin, R., Moniatte, M., Dorin-Semblat, D., Spicer, J. A., Srivastava, A., Retzlaff, S., Heussler, V., Waters, A. P., & Doerig, C. (2011). Activation of a PAK-MEK signalling pathway in malaria parasite-infected erythrocytes. Cellular Microbiology, 13(6), 836-845. https://doi.org/10.1111/j.1462-5822.2011.01582.x
Silvie, O., Rubinstein, E., Franetich, J.-F., Prenant, M., Belnoue, E., Rénia, L., Hannoun, L., Eling, W., Levy, S., Boucheix, C., & Mazier, D. (2003). Hepatocyte CD81 is required for Plasmodium falciparum and Plasmodium yoelii sporozoite infectivity. Nature Medicine, 9(1), 93-96. https://doi.org/10.1038/nm808
Singh, A. P., Zhang, Y., No, J.-H., Docampo, R., Nussenzweig, V., & Oldfield, E. (2010). Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth. Antimicrobial Agents and Chemotherapy, 54(7), 2987-2993. https://doi.org/10.1128/AAC.00198-10
Sinigaglia, L., Varenna, M., & Casari, S. (2007). Pharmacokinetic profile of bisphosphonates in the treatment of metabolic bone disorders. Clinical Cases in Mineral and Bone Metabolism: The Official Journal of the Italian Society of Osteoporosis, Mineral Metabolism, and Skeletal Diseases, 4(1), 30-36.
Sinxadi, P., Donini, C., Johnstone, H., Langdon, G., Wiesner, L., Allen, E., Duparc, S., Chalon, S., McCarthy, J. S., Lorch, U., Chibale, K., Möhrle, J., & Barnes, K. I. (2020). Safety, tolerability, pharmacokinetics, and antimalarial activity of the novel Plasmodium phosphatidylinositol 4-kinase inhibitor MMV390048 in healthy volunteers. Antimicrobial Agents and Chemotherapy, 64(4), e01896-19. https://doi.org/10.1128/AAC.01896-19
Sleebs, B. E., Gazdik, M., O'Neill, M. T., Rajasekaran, P., Lopaticki, S., Lackovic, K., Lowes, K., Smith, B. J., Cowman, A. F., & Boddey, J. A. (2014). Transition state mimetics of the Plasmodium export element are potent inhibitors of plasmepsin V from P. falciparum and P. vivax. Journal of Medicinal Chemistry, 57(18), 7644-7662. https://doi.org/10.1021/jm500797g
Song, Z., Iorga, B. I., Mounkoro, P., Fisher, N., & Meunier, B. (2018). The antimalarial compound ELQ-400 is an unusual inhibitor of the bc1 complex, targeting both Qo and Qi sites. FEBS Letters, 592(8), 1346-1356. https://doi.org/10.1002/1873-3468.13035
Sonoiki, E., Ng, C. L., Lee, M. C. S., Guo, D., Zhang, Y.-K., Zhou, Y., Alley, M. R. K., Ahyong, V., Sanz, L. M., Lafuente-Monasterio, M. J., Dong, C., Schupp, P. G., Gut, J., Legac, J., Cooper, R. A., Gamo, F.-J., DeRisi, J., Freund, Y. R., Fidock, D. A., & Rosenthal, P. J. (2017). A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue. Nature Communications, 8, 14574. https://doi.org/10.1038/ncomms14574
Spahn, C. M. T., Gomez-Lorenzo, M. G., Grassucci, R. A., Jørgensen, R., Andersen, G. R., Beckmann, R., Penczek, P. A., Ballesta, J. P. G., & Frank, J. (2004). Domain movements of elongation factor eEF2 and the eukaryotic 80S ribosome facilitate tRNA translocation. The EMBO Journal, 23(5), 1008-1019. https://doi.org/10.1038/sj.emboj.7600102
Spillman, N. J., Allen, R. J., McNamara, C. W., Yeung, B. K., Winzeler, E. A., Diagana, T. T., & Kirk, K. (2013). Na(+) regulation in the malaria parasite Plasmodium falciparum involves the cation ATPase PfATP4 and is a target of the spiroindolone antimalarials. Cell Host & Microbe, 13(2), 227-237. https://doi.org/10.1016/j.chom.2012.12.006
Srivastava, I. K., Rottenberg, H., & Vaidya, A. B. (1997). Atovaquone, a broad spectrum antiparasitic drug, collapses mitochondrial membrane potential in a malarial parasite. The Journal of Biological Chemistry, 272(7), 3961-3966. https://doi.org/10.1074/jbc.272.7.3961
Srivastava, I. K., & Vaidya, A. B. (1999). A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrobial Agents and Chemotherapy, 43(6), 1334-1339.
Srivastava, S., Bhowmick, K., Chatterjee, S., Basha, J., Kundu, T. K., & Dhar, S. K. (2014). Histone H3K9 acetylation level modulates gene expression and may affect parasite growth in human malaria parasite Plasmodium falciparum. The FEBS Journal, 281(23), 5265-5278. https://doi.org/10.1111/febs.13067
Sternberg, A. R., & Roepe, P. D. (2020). Heterologous expression, purification, and functional analysis of the Plasmodium falciparum phosphatidylinositol 4-kinase IIIβ. Biochemistry, 59(27), 2494-2506. https://doi.org/10.1021/acs.biochem.0c00259
Stickles, A. M., de Almeida, M. J., Morrisey, J. M., Sheridan, K. A., Forquer, I. P., Nilsen, A., Winter, R. W., Burrows, J. N., Fidock, D. A., Vaidya, A. B., & Riscoe, M. K. (2015). Subtle changes in endochin-like quinolone structure alter the site of inhibition within the cytochrome bc1 complex of Plasmodium falciparum. Antimicrobial Agents and Chemotherapy, 59(4), 1977-1982. https://doi.org/10.1128/AAC.04149-14
Stickles, A. M., Smilkstein, M. J., Morrisey, J. M., Li, Y., Forquer, I. P., Kelly, J. X., Pou, S., Winter, R. W., Nilsen, A., Vaidya, A. B., & Riscoe, M. K. (2016). Atovaquone and ELQ-300 combination therapy as a novel dual-site cytochrome bc1 inhibition strategy for malaria. Antimicrobial Agents and Chemotherapy, 60(8), 4853-4859. https://doi.org/10.1128/AAC.00791-16
Stokes, B. H., Yoo, E., Murithi, J. M., Luth, M. R., Afanasyev, P., da Fonseca, P. C. A., Winzeler, E. A., Ng, C. L., Bogyo, M., & Fidock, D. A. (2019). Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple antimalarial agents. PLoS Pathogens, 15(6), e1007722. https://doi.org/10.1371/journal.ppat.1007722
Sturm, A., Mollard, V., Cozijnsen, A., Goodman, C. D., & McFadden, G. I. (2015). Mitochondrial ATP synthase is dispensable in blood-stage Plasmodium berghei rodent malaria but essential in the mosquito phase. Proceedings of the National Academy of Sciences of the United States of America, 112(33), 10216-10223. https://doi.org/10.1073/pnas.1423959112
Sun, W., Tanaka, T. Q., Magle, C. T., Huang, W., Southall, N., Huang, R., Dehdashti, S. J., McKew, J. C., Williamson, K. C., & Zheng, W. (2014). Chemical signatures and new drug targets for gametocytocidal drug development. Scientific Reports, 4, 3743. https://doi.org/10.1038/srep03743
Swale, C., Bougdour, A., Gnahoui-David, A., Tottey, J., Georgeault, S., Laurent, F., Palencia, A., & Hakimi, M.-A. (2019). Metal-captured inhibition of pre-mRNA processing activity by CPSF3 controls Cryptosporidium infection. Science Translational Medicine, 11(517), eaax7161. https://doi.org/10.1126/scitranslmed.aax7161
Taft, B. R., Yokokawa, F., Kirrane, T., Mata, A.-C., Huang, R., Blaquiere, N., Waldron, G., Zou, B., Simon, O., Vankadara, S., Chan, W. L., Ding, M., Sim, S., Straimer, J., Guiguemde, A., Lakshminarayana, S. B., Jain, J. P., Bodenreider, C., Thompson, C., … Sarko, C. (2022). Discovery and preclinical pharmacology of INE963, a potent and fast-acting blood-stage antimalarial with a high barrier to resistance and potential for single-dose cures in uncomplicated malaria. Journal of Medicinal Chemistry, 65(5), 3798-3813. https://doi.org/10.1021/acs.jmedchem.1c01995
Tawk, L., Chicanne, G., Dubremetz, J.-F., Richard, V., Payrastre, B., Vial, H. J., Roy, C., & Wengelnik, K. (2010). Phosphatidylinositol 3-phosphate, an essential lipid in Plasmodium, localizes to the food vacuole membrane and the apicoplast. Eukaryotic Cell, 9(10), 1519-1530. https://doi.org/10.1128/EC.00124-10
Taylor, H. M., McRobert, L., Grainger, M., Sicard, A., Dluzewski, A. R., Hopp, C. S., Holder, A. A., & Baker, D. A. (2010). The malaria parasite cyclic GMP-dependent protein kinase plays a central role in blood-stage schizogony. Eukaryotic Cell, 9(1), 37-45. https://doi.org/10.1128/EC.00186-09
Taylor, N. (1943). Quinine: The story of cinchona. The Scientific Monthly, 57(1), 17-32. JSTOR.
Taylor, W. R. J., & White, N. J. (2004). Antimalarial drug toxicity: A review. Drug Safety, 27(1), 25-61. https://doi.org/10.2165/00002018-200427010-00003
Tewari, R., Straschil, U., Bateman, A., Böhme, U., Cherevach, I., Gong, P., Pain, A., & Billker, O. (2010). The systematic functional analysis of Plasmodium protein kinases identifies essential regulators of mosquito transmission. Cell Host & Microbe, 8(4), 377-387. https://doi.org/10.1016/j.chom.2010.09.006
Tickell-Painter, M., Maayan, N., Saunders, R., Pace, C., & Sinclair, D. (2017). Mefloquine for preventing malaria during travel to endemic areas. The Cochrane Database of Systematic Reviews, 10, CD006491. https://doi.org/10.1002/14651858.CD006491.pub4
Toé, K. H., Jones, C. M., N'Fale, S., Ismail, H. M., Dabiré, R. K., & Ranson, H. (2014). Increased pyrethroid resistance in malaria vectors and decreased bed net effectiveness, Burkina Faso. Emerging Infectious Diseases, 20(10), 1691-1696. https://doi.org/10.3201/eid2010.140619
Tonkin, C. J., Carret, C. K., Duraisingh, M. T., Voss, T. S., Ralph, S. A., Hommel, M., Duffy, M. F., da Silva, L. M., Scherf, A., Ivens, A., Speed, T. P., Beeson, J. G., & Cowman, A. F. (2009). Sir2 paralogues cooperate to regulate virulence genes and antigenic variation in Plasmodium falciparum. PLoS Biology, 7(4), e84. https://doi.org/10.1371/journal.pbio.1000084
Tsagris, D. J., Birchall, K., Bouloc, N., Large, J. M., Merritt, A., Smiljanic-Hurley, E., Wheldon, M., Ansell, K. H., Kettleborough, C., Whalley, D., Stewart, L. B., Bowyer, P. W., Baker, D. A., & Osborne, S. A. (2018). Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG). Bioorganic & Medicinal Chemistry Letters, 28(19), 3168-3173. https://doi.org/10.1016/j.bmcl.2018.08.028
Tuju, J., Kamuyu, G., Murungi, L. M., & Osier, F. H. A. (2017). Vaccine candidate discovery for the next generation of malaria vaccines. Immunology, 152(2), 195-206. https://doi.org/10.1111/imm.12780
Tye, M. A., Payne, N. C., Johansson, C., Singh, K., Santos, S. A., Fagbami, L., Pant, A., Sylvester, K., Luth, M. R., Marques, S., Whitman, M., Mota, M. M., Winzeler, E. A., Lukens, A. K., Derbyshire, E. R., Oppermann, U., Wirth, D. F., & Mazitschek, R. (2022). Elucidating the path to Plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance. Nature Communications, 13(1), 4976. https://doi.org/10.1038/s41467-022-32630-4
Vaidya, A. B., & Mather, M. W. (2000). Atovaquone resistance in malaria parasites. Drug Resistance Updates: Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy, 3(5), 283-287. https://doi.org/10.1054/drup.2000.0157
Vaidya, A. B., Morrisey, J. M., Zhang, Z., Das, S., Daly, T. M., Otto, T. D., Spillman, N. J., Wyvratt, M., Siegl, P., Marfurt, J., Wirjanata, G., Sebayang, B. F., Price, R. N., Chatterjee, A., Nagle, A., Stasiak, M., Charman, S. A., Angulo-Barturen, I., Ferrer, S., … Bergman, L. W. (2014). Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum. Nature Communications, 5, 5521. https://doi.org/10.1038/ncomms6521
van der Pluijm, R. W., Amaratunga, C., Dhorda, M., & Dondorp, A. M. (2021). Triple artemisinin-based combination therapies for malaria-A new paradigm? Trends in Parasitology, 37(1), 15-24. https://doi.org/10.1016/j.pt.2020.09.011
van Pelt-Koops, J. C., Pett, H. E., Graumans, W., van der Vegte-Bolmer, M., van Gemert, G. J., Rottmann, M., Yeung, B. K. S., Diagana, T. T., & Sauerwein, R. W. (2012). The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vector. Antimicrobial Agents and Chemotherapy, 56(7), 3544-3548. https://doi.org/10.1128/AAC.06377-11
van Schaijk, B. C. L., Kumar, T. R. S., Vos, M. W., Richman, A., van Gemert, G.-J., Li, T., Eappen, A. G., Williamson, K. C., Morahan, B. J., Fishbaugher, M., Kennedy, M., Camargo, N., Khan, S. M., Janse, C. J., Sim, K. L., Hoffman, S. L., Kappe, S. H. I., Sauerwein, R. W., Fidock, D. A., & Vaughan, A. M. (2014). Type II fatty acid biosynthesis is essential for Plasmodium falciparum sporozoite development in the midgut of Anopheles mosquitoes. Eukaryotic Cell, 13(5), 550-559. https://doi.org/10.1128/EC.00264-13
Vanaerschot, M., Murithi, J. M., Pasaje, C. F. A., Ghidelli-Disse, S., Dwomoh, L., Bird, M., Spottiswoode, N., Mittal, N., Arendse, L. B., Owen, E. S., Wicht, K. J., Siciliano, G., Bösche, M., Yeo, T., Kumar, T. R. S., Mok, S., Carpenter, E. F., Giddins, M. J., Sanz, O., … Fidock, D. A. (2020). Inhibition of resistance-refractory P. falciparum kinase PKG delivers prophylactic, blood stage, and transmission-blocking antiplasmodial activity. Cell Chemical Biology, 27(7), 806-816.e8. https://doi.org/10.1016/j.chembiol.2020.04.001
Vanheer, L. N., Zhang, H., Lin, G., & Kafsack, B. F. C. (2020). Activity of epigenetic inhibitors against Plasmodium falciparum asexual and sexual blood stages. Antimicrobial Agents and Chemotherapy, 64(7), e02523-19. https://doi.org/10.1128/AAC.02523-19
Vos, M. W., Stone, W. J. R., Koolen, K. M., van Gemert, G.-J., van Schaijk, B., Leroy, D., Sauerwein, R. W., Bousema, T., & Dechering, K. J. (2015). A semi-automated luminescence based standard membrane feeding assay identifies novel small molecules that inhibit transmission of malaria parasites by mosquitoes. Scientific Reports, 5, 18704. https://doi.org/10.1038/srep18704
Wagner, M. P., Formaglio, P., Gorgette, O., Dziekan, J. M., Huon, C., Berneburg, I., Rahlfs, S., Barale, J.-C., Feinstein, S. I., Fisher, A. B., Ménard, D., Bozdech, Z., Amino, R., Touqui, L., & Chitnis, C. E. (2022). Human peroxiredoxin 6 is essential for malaria parasites and provides a host-based drug target. Cell Reports, 39(11), 110923. https://doi.org/10.1016/j.celrep.2022.110923
Wall, R. J., Rico, E., Lukac, I., Zuccotto, F., Elg, S., Gilbert, I. H., Freund, Y., Alley, M. R. K., Field, M. C., Wyllie, S., & Horn, D. (2018). Clinical and veterinary trypanocidal benzoxaboroles target CPSF3. Proceedings of the National Academy of Sciences of the United States of America, 115(38), 9616-9621. https://doi.org/10.1073/pnas.1807915115
Wang, J., Xu, C., Wong, Y. K., Li, Y., Liao, F., Jiang, T., & Tu, Y. (2019). Artemisinin, the magic drug discovered from traditional Chinese medicine. Engineering, 5(1), 32-39. https://doi.org/10.1016/j.eng.2018.11.011
Wang, M., Tang, T., Li, R., Huang, Z., Ling, D., Zheng, L., Ding, Y., Liu, T., Xu, W., Zhu, F., Min, H., Boonhok, R., Mao, F., Zhu, J., Li, X., Jiang, L., & Li, J. (2022). Drug repurposing of quisinostat to discover novel Plasmodium falciparum HDAC1 inhibitors with enhanced triple-stage antimalarial activity and improved safety. Journal of Medicinal Chemistry, 65, 4156-4181. https://doi.org/10.1021/acs.jmedchem.1c01993
Ward, P., Equinet, L., Packer, J., & Doerig, C. (2004). Protein kinases of the human malaria parasite Plasmodium falciparum: The kinome of a divergent eukaryote. BMC Genomics, 5, 79. https://doi.org/10.1186/1471-2164-5-79
White, J., Dhingra, S. K., Deng, X., El Mazouni, F., Lee, M. C. S., Afanador, G. A., Lawong, A., Tomchick, D. R., Ng, C. L., Bath, J., Rathod, P. K., Fidock, D. A., & Phillips, M. A. (2019). Identification and mechanistic understanding of dihydroorotate dehydrogenase point mutations in Plasmodium falciparum that confer in vitro resistance to the clinical candidate DSM265. ACS Infectious Diseases, 5(1), 90-101. https://doi.org/10.1021/acsinfecdis.8b00211
White, N. J. (1999). Delaying antimalarial drug resistance with combination chemotherapy. Parassitologia, 41(1-3), 301-308.
Woodrow, C. J., Haynes, R. K., & Krishna, S. (2005). Artemisinins. Postgraduate Medical Journal, 81(952), 71-78. https://doi.org/10.1136/pgmj.2004.028399
World Health Organization. (2021). World malaria report 2021. World Health Organization. https://apps.who.int/iris/handle/10665/350147
Wright, M. H., Clough, B., Rackham, M. D., Rangachari, K., Brannigan, J. A., Grainger, M., Moss, D. K., Bottrill, A. R., Heal, W. P., Broncel, M., Serwa, R. A., Brady, D., Mann, D. J., Leatherbarrow, R. J., Tewari, R., Wilkinson, A. J., Holder, A. A., & Tate, E. W. (2014). Validation of N-myristoyltransferase as an antimalarial drug target using an integrated chemical biology approach. Nature Chemistry, 6(2), 112-121. https://doi.org/10.1038/nchem.1830
Wright, M. H., Heal, W. P., Mann, D. J., & Tate, E. W. (2010). Protein myristoylation in health and disease. Journal of Chemical Biology, 3(1), 19-35. https://doi.org/10.1007/s12154-009-0032-8
Xie, S. C., Gillett, D. L., Spillman, N. J., Tsu, C., Luth, M. R., Ottilie, S., Duffy, S., Gould, A. E., Hales, P., Seager, B. A., Charron, C. L., Bruzzese, F., Yang, X., Zhao, X., Huang, S.-C., Hutton, C. A., Burrows, J. N., Winzeler, E. A., Avery, V. M., … Tilley, L. (2018). Target validation and identification of novel boronate inhibitors of the Plasmodium falciparum proteasome. Journal of Medicinal Chemistry, 61(22), 10053-10066. https://doi.org/10.1021/acs.jmedchem.8b01161
Xie, S. C., Metcalfe, R. D., Dunn, E., Morton, C. J., Huang, S.-C., Puhalovich, T., Du, Y., Wittlin, S., Nie, S., Luth, M. R., Ma, L., Kim, M.-S., Pasaje, C. F. A., Kumpornsin, K., Giannangelo, C., Houghton, F. J., Churchyard, A., Famodimu, M. T., Barry, D. C., … Tilley, L. (2022). Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy. Science (New York, N.Y.), 376(6597), 1074-1079. https://doi.org/10.1126/science.abn0611
Yahiya, S., Rueda-Zubiaurre, A., Delves, M. J., Fuchter, M. J., & Baum, J. (2019). The antimalarial screening landscape-looking beyond the asexual blood stage. Current Opinion in Chemical Biology, 50, 1-9. https://doi.org/10.1016/j.cbpa.2019.01.029
Yanagisawa, T., Lee, J. T., Wu, H. C., & Kawakami, M. (1994). Relationship of protein structure of isoleucyl-tRNA synthetase with pseudomonic acid resistance of Escherichia coli. A proposed mode of action of pseudomonic acid as an inhibitor of isoleucyl-tRNA synthetase. The Journal of Biological Chemistry, 269(39), 24304-24309.
Yang, T., Ottilie, S., Istvan, E. S., Godinez-Macias, K. P., Lukens, A. K., Baragaña, B., Campo, B., Walpole, C., Niles, J. C., Chibale, K., Dechering, K. J., Llinás, M., Lee, M. C. S., Kato, N., Wyllie, S., McNamara, C. W., Gamo, F. J., Burrows, J., Fidock, D. A., … Malaria Drug Accelerator Consortium. (2021). MalDA, accelerating malaria drug discovery. Trends in Parasitology, 37(6), 493-507. https://doi.org/10.1016/j.pt.2021.01.009
Yoo, E., Stokes, B. H., de Jong, H., Vanaerschot, M., Kumar, T., Lawrence, N., Njoroge, M., Garcia, A., Van der Westhuyzen, R., Momper, J. D., Ng, C. L., Fidock, D. A., & Bogyo, M. (2018). Defining the determinants of specificity of Plasmodium proteasome inhibitors. Journal of the American Chemical Society, 140(36), 11424-11437. https://doi.org/10.1021/jacs.8b06656
Yu, Z., Brannigan, J. A., Moss, D. K., Brzozowski, A. M., Wilkinson, A. J., Holder, A. A., Tate, E. W., & Leatherbarrow, R. J. (2012). Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery. Journal of Medicinal Chemistry, 55(20), 8879-8890. https://doi.org/10.1021/jm301160h
Yu, Z., Brannigan, J. A., Rangachari, K., Heal, W. P., Wilkinson, A. J., Holder, A. A., Leatherbarrow, R. J., & Tate, E. W. (2015). Discovery of pyridyl-based inhibitors of Plasmodium falciparum N-myristoyltransferase. MedChemComm, 6(10), 1767-1772. https://doi.org/10.1039/c5md00242g
Yuthavong, Y., Tarnchompoo, B., Vilaivan, T., Chitnumsub, P., Kamchonwongpaisan, S., Charman, S. A., McLennan, D. N., White, K. L., Vivas, L., Bongard, E., Thongphanchang, C., Taweechai, S., Vanichtanankul, J., Rattanajak, R., Arwon, U., Fantauzzi, P., Yuvaniyama, J., Charman, W. N., & Matthews, D. (2012). Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target. Proceedings of the National Academy of Sciences, 109, 16823-16828. https://doi.org/10.1073/pnas.1204556109
Yuthavong, Y., Yuvaniyama, J., Chitnumsub, P., Vanichtanankul, J., Chusacultanachai, S., Tarnchompoo, B., Vilaivan, T., & Kamchonwongpaisan, S. (2005). Malarial (Plasmodium falciparum) dihydrofolate reductase-thymidylate synthase: Structural basis for antifolate resistance and development of effective inhibitors. Parasitology, 130(Pt 3), 249-259. https://doi.org/10.1017/s003118200400664x
Yuvaniyama, J., Chitnumsub, P., Kamchonwongpaisan, S., Vanichtanankul, J., Sirawaraporn, W., Taylor, P., Walkinshaw, M. D., & Yuthavong, Y. (2003). Insights into antifolate resistance from malarial DHFR-TS structures. Nature Structural Biology, 10(5), 357-365. https://doi.org/10.1038/nsb921
Zhang, M., Wang, C., Otto, T. D., Oberstaller, J., Liao, X., Adapa, S. R., Udenze, K., Bronner, I. F., Casandra, D., Mayho, M., Brown, J., Li, S., Swanson, J., Rayner, J. C., Jiang, R. H. Y., & Adams, J. H. (2018). Uncovering the essential genes of the human malaria parasite Plasmodium falciparum by saturation mutagenesis. Science (New York, N.Y.), 360(6388), eaap7847. https://doi.org/10.1126/science.aap7847