Utilization of an optimized AlphaFold protein model for structure-based design of a selective HDAC11 inhibitor with anti-neuroblastoma activity.

AlphaFold HDAC11 model optimization molecular dynamics simulation neuroblastoma

Journal

Archiv der Pharmazie
ISSN: 1521-4184
Titre abrégé: Arch Pharm (Weinheim)
Pays: Germany
ID NLM: 0330167

Informations de publication

Date de publication:
12 Jul 2024
Historique:
revised: 26 06 2024
received: 14 06 2024
accepted: 27 06 2024
medline: 12 7 2024
pubmed: 12 7 2024
entrez: 12 7 2024
Statut: aheadofprint

Résumé

AlphaFold is an artificial intelligence approach for predicting the three-dimensional (3D) structures of proteins with atomic accuracy. One challenge that limits the use of AlphaFold models for drug discovery is the correct prediction of folding in the absence of ligands and cofactors, which compromises their direct use. We have previously described the optimization and use of the histone deacetylase 11 (HDAC11) AlphaFold model for the docking of selective inhibitors such as FT895 and SIS17. Based on the predicted binding mode of FT895 in the optimized HDAC11 AlphaFold model, a new scaffold for HDAC11 inhibitors was designed, and the resulting compounds were tested in vitro against various HDAC isoforms. Compound 5a proved to be the most active compound with an IC

Identifiants

pubmed: 38996352
doi: 10.1002/ardp.202400486
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

e2400486

Subventions

Organisme : Deutsche Forschungsgemeinschaft (DFG)
ID : 469954457
Organisme : Deutsche Forschungsgemeinschaft (DFG)
ID : 471614207
Organisme : CAS
ID : 86652036
Organisme : Grant Agency of the Czech Republic
ID : 24-12155 S

Informations de copyright

© 2024 The Author(s). Archiv der Pharmazie published by Wiley‐VCH GmbH on behalf of Deutsche Pharmazeutische Gesellschaft.

Références

P. M. Lombardi, K. E. Cole, D. P. Dowling, D. W. Christianson, Curr. Opin. Struct. Biol. 2011, 21(6), 735.
M. Marek, T. B. Shaik, C. Romier Epigenetic Drug Discovery (Eds W. Sippl, M. Jung), Wiley‐VCH Verlag GmbH & Co. KGaA, Boschstr, 12, 69469 Weinheim, Germany 2019, pp. 11Chapter 2.
H. Chen, C. Xie, Q. Chen, S. Zhuang, Front. Endocrinol. 2022, 13, 989305.
S. S. Liu, F. Wu, Y. M. Jin, W. Q. Chang, T. M. Xu, Biomed. Pharmacother. 2020, 131, 110607.
H. E. Deubzer, M. C. Schier, I. Oehme, M. Lodrini, B. Haendler, A. Sommer, O. Witt, Int. J. Cancer 2013, 132(9), 2200.
D. Gong, Z. Zeng, F. Yi, J. Wu, Am. J. Transl. Res. 2019, 11(2), 983.
W. Huo, F. Qi, K. Wang, Oncol. Rep. 2020, 44(3), 1233.
W. Wang, L. Fu, S. Li, Z. Xu, X. Li, Cell Biol. Int. 2017, 41(12), 1290.
M. W. Martin, J. Y. Lee, D. R. Lancia, P. Y. Ng, B. Han, J. R. Thomason, M. S. Lynes, C. G. Marshall, C. Conti, A. Collis, M. A. Morales, K. Doshi, A. Rudnitskaya, L. Yao, X. Zheng, Bioorg. Med. Chem. Lett. 2018, 28(12), 2143.
N. Bora‐Singhal, D. Mohankumar, B. Saha, C. M. Colin, J. Y. Lee, M. W. Martin, X. Zheng, D. Coppola, S. Chellappan, Sci. Rep. 2020, 10(1), 4722.
P. Bai, Y. Liu, L. Yang, W. Ding, P. Mondal, N. Sang, G. Liu, X. Lu, T. T. Ho, Y. Zhou, R. Wu, V. C. Birar, M. Q. Wilks, R. E. Tanzi, H. Lin, C. Zhang, W. Li, S. Shen, C. Wang, J. Med. Chem. 2023, 66(23), 16075.
Z. Kutil, J. Mikešová, M. Zessin, M. Meleshin, Z. Nováková, G. Alquicer, A. Kozikowski, W. Sippl, C. Bařinka, M. Schutkowski, ACS Omega 2019, 4(22), 19895.
Z. Kutil, Z. Novakova, M. Meleshin, J. Mikesova, M. Schutkowski, C. Barinka, ACS Chem. Biol. 2018, 13(3), 685.
S. I. Son, J. Cao, C.‐L. Zhu, S. P. Miller, H. Lin, ACS Chem. Biol. 2019, 14(7), 1393.
T. T. Ho, C. Peng, E. Seto, H. Lin, ACS Chem. Biol. 2023, 18(4), 803.
F. Baselious, D. Robaa, W. Sippl, Comput. Biol. Med. 2023, 167, 107700.
L. Gao, M. A. Cueto, F. Asselbergs, P. Atadja, J. Biol. Chem. 2002, 277(28), 25748.
J. Jumper; R. Evans; A. Pritzel; T. Green; M. Figurnov; O. Ronneberger; K. Tunyasuvunakool; R. Bates; A. Žídek; A. Potapenko; A. Bridgland; C. Meyer; S. a. A. Kohl; A. J. Ballard; A. Cowie; B. Romera‐Paredes; S. Nikolov; R. Jain; J. Adler; T. Back; S. Petersen; D. Reiman; E. Clancy; M. Zielinski; M. Steinegger; M. Pacholska; T. Berghammer; S. Bodenstein; D. Silver; O. Vinyals; A. W. Senior; K. Kavukcuoglu; P. Kohli; D. Hassabis, Nature 2021, 596(7873), 583.
A. David, S. Islam, E. Tankhilevich, M. J. E. Sternberg, J. Mol. Biol. 2022, 434(2), 167336.
F. Ren; X. Ding; M. Zheng; M. Korzinkin; X. Cai; W. Zhu; A. Mantsyzov; A. Aliper; V. Aladinskiy; Z. Cao; S. Kong; X. Long; B. H. Man Liu; Y. Liu; V. Naumov; A. Shneyderman; I. V. Ozerov; J. Wang; F. W. Pun; D. A. Polykovskiy; C. Sun; M. Levitt; A. Aspuru‐Guzik; A. Zhavoronkov, Chem. Sci. 2023, 14(6), 1443.
W. Zhu; X. Liu; Q. Li; F. Gao; T. Liu; X. Chen; M. Zhang; A. Aliper; F. Ren; X. Ding; A. Zhavoronkov, Bioorg. Med. Chem. 2023, 91, 117414.
A. M. Díaz‐Rovira, H. Martín, T. Beuming, L. Díaz, V. Guallar, S. S. Ray, J. Chem. Inf. Model. 2023, 63(6), 1668.
X. He, C. You, H. Jiang, Y. Jiang, H. E. Xu, X. Cheng, Acta Pharmacol. Sin. 2023, 44(1), 1.
M. Holcomb, Y. T. Chang, D. S. Goodsell, S. Forli, Protein Sci. 2023, 32(1), e4530.
V. Scardino, J. I. Di Filippo, C. N. Cavasotto, iScience 2023, 26(1), 105920.
M. Karelina, J. J. Noh, R. O. Dror, eLife 2023, 12, RP89386.
F. Baselious, S. Hilscher, D. Robaa, C. Barinka, M. Schutkowski, W. Sippl, Int. J. Mol. Sci. 2024, 25(2), c1358.
N. S. M. Ismail, R. F. George, R. aT. Serya, F. N. Baselious, M. El‐Manawaty, E. M. Shalaby, A. S. Girgis, RSC Adv. 2016, 6(104), 101911.
T. M. Thole, M. Lodrini, J. Fabian, J. Wuenschel, S. Pfeil, T. Hielscher, A. Kopp‐Schneider, U. Heinicke, S. Fulda, O. Witt, A. Eggert, M. Fischer, H. E. Deubzer, Cell Death Dis. 2017, 8(3), e2635.
E. F. Bülbül, J. Melesina, H. S. Ibrahim, M. Abdelsalam, A. Vecchio, D. Robaa, M. Zessin, M. Schutkowski, W. Sippl, Molecules 2022, 27(8), 2526.
J. Liu, Y. Yu, J. Kelly, D. Sha, A.‐B. Alhassan, W. Yu, M. M. Maletic, J. L. Duffy, D. J. Klein, M. K. Holloway, S. Carroll, B. J. Howell, R. J. O. Barnard, S. Wolkenberg, J. A. Kozlowski, ACS Med. Chem. Lett. 2020, 11(12), 2476.
L. Whitehead, M. R. Dobler, B. Radetich, Y. Zhu, P. W. Atadja, T. Claiborne, J. E. Grob, A. Mcriner, M. R. Pancost, A. Patnaik, W. Shao, M. Shultz, R. Tichkule, R. A. Tommasi, B. Vash, P. Wang, T. Stams, Bioorg. Med. Chem. 2011, 19(15), 4626.
Schrödinger Release 2019‐1: Maestro, Schrödinger, LLC, New York, NY, 2019.
Schrödinger Release 2019‐1: Protein Preparation Wizard. Epik, Schrödinger, LLC, New York, NY, 2019; Impact, Schrödinger, LLC, New York, NY, 2019; Prime, Schrödinger, LLC, New York, NY, 2019.
G. Madhavi Sastry, M. Adzhigirey, T. Day, R. Annabhimoju, W. Sherman., J. Comput.‐Aided Mol. Des. 2013, 27(3), 221.
Schrödinger Release 2019‐1: Epik, Schrödinger, LLC, New York, NY, 2019.
J. R. Greenwood, D. Calkins, A. P. Sullivan, J. C. Shelley, J. Comput.‐Aided Mol. Des. 2010, 24(6–7), 591.
J. C. Shelley, A. Cholleti, L. L. Frye, J. R. Greenwood, M. R. Timlin, M. Uchimaya, J. Comput.‐Aided Mol. Des. 2007, 21(12), 681.
E. Ghazy, T. Heimburg, J. Lancelot, P. Zeyen, K. Schmidtkunz, A. Truhn, S. Darwish, C. V. Simoben, T. B. Shaik, F. Erdmann, M. Schmidt, D. Robaa, C. Romier, M. Jung, R. Pierce, W. Sippl, Eur. J. Med. Chem. 2021, 225, 113745.
E. Ghazy, P. Zeyen, D. Herp, M. Hügle, K. Schmidtkunz, F. Erdmann, D. Robaa, M. Schmidt, E. R. Morales, C. Romier, S. Günther, M. Jung, W. Sippl, Eur. J. Med. Chem. 2020, 200, 112338.
M. Marek, T. B. Shaik, T. Heimburg, A. Chakrabarti, J. Lancelot, E. Ramos‐Morales, C. Da Veiga, D. Kalinin, J. Melesina, D. Robaa, K. Schmidtkunz, T. Suzuki, R. Holl, E. Ennifar, R. J. Pierce, M. Jung, W. Sippl, C. Romier, J. Med. Chem. 2018, 61(22), 10000.
K. Vögerl, N. Ong, J. Senger, D. Herp, K. Schmidtkunz, M. Marek, M. Müller, K. Bartel, T. B. Shaik, N. J. Porter, D. Robaa, D. W. Christianson, C. Romier, W. Sippl, M. Jung, F. Bracher, J. Med. Chem. 2019, 62(3), 1138.
Schrödinger Release 2019‐1: LigPrep, Schrödinger, LLC, New York, NY, 2019.
E. Harder, W. Damm, J. Maple, C. Wu, M. Reboul, J. Y. Xiang, L. Wang, D. Lupyan, M. K. Dahlgren, J. L. Knight, J. W. Kaus, D. S. Cerutti, G. Krilov, W. L. Jorgensen, R. Abel, R. A. Friesner, J. Chem. Theory Comput. 2016, 12(1), 281.
W. L. Jorgensen, D. S. Maxwell, J. Tirado‐Rives, J. Am. Chem. Soc. 1996, 118(45), 11225.
W. L. Jorgensen, J. Tirado‐Rives, J. Am. Chem. Soc. 1988, 110(6), 1657.
D. Shivakumar, J. Williams, Y. Wu, W. Damm, J. Shelley, W. Sherman, J. Chem. Theory Comput. 2010, 6(5), 1509.
Schrödinger Release 2019‐1: Glide, Schrödinger, LLC, New York, NY, 2019.
R. A. Friesner, J. L. Banks, R. B. Murphy, T. A. Halgren, J. J. Klicic, D. T. Mainz, M. P. Repasky, E. H. Knoll, M. Shelley, J. K. Perry, D. E. Shaw, P. Francis, P. S. Shenkin, J. Med. Chem. 2004, 47(7), 1739.
R. A. Friesner, R. B. Murphy, M. P. Repasky, L. L. Frye, J. R. Greenwood, T. A. Halgren, P. C. Sanschagrin, D. T. Mainz, J. Med. Chem. 2006, 49(21), 6177.
T. A. Halgren, R. B. Murphy, R. A. Friesner, H. S. Beard, L. L. Frye, W. T. Pollard, J. L. Banks, J. Med. Chem. 2004, 47(7), 1750.
Schrödinger Release 2019‐1. Desmond Molecular Dynamics System, D.E. Shaw Research, New York, NY, 2019, Maestro‐Desmond Interoperability Tools, Schrödinger, New York, NY, USA 2019.
K. J. Bowers, D. E. Chow, H. Xu, R. O. Dror, M. P. Eastwood, B. A. Gregersen, J. L. Klepeis, I. Kolossvary, M. A. Moraes, F. D. Sacerdoti, J. K. Salmon, Y. Shan, D. E. Shaw. Scalable algorithms for molecular dynamics simulations on commodity clusters. In Proceedings of the 2006 ACM/IEEE Conference on Supercomputing, 11‐ 17 Nov. 2006, Tampa, FL, USA 2006. p.43. https://doi.org/10.1109/SC.2006.54
M. Zessin, Z. Kutil, M. Meleshin, Z. Nováková, E. Ghazy, D. Kalbas, M. Marek, C. Romier, W. Sippl, C. Bařinka, M. Schutkowski, Biochemistry 2019, 58(48), 4777.
T. Heimburg, F. R. Kolbinger, P. Zeyen, E. Ghazy, D. Herp, K. Schmidtkunz, J. Melesina, T. B. Shaik, F. Erdmann, M. Schmidt, C. Romier, D. Robaa, O. Witt, I. Oehme, M. Jung, W. Sippl, J. Med. Chem. 2017, 60(24), 10188.

Auteurs

Fady Baselious (F)

Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, Halle (Saale), Germany.

Sebastian Hilscher (S)

Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, Halle (Saale), Germany.

Sven Hagemann (S)

Institute of Molecular Medicine, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany.

Sunita Tripathee (S)

Institute of Molecular Medicine, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany.

Dina Robaa (D)

Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, Halle (Saale), Germany.

Cyril Barinka (C)

Institute of Biotechnology of the Czech Academy of Sciences, BIOCEV, Vestec, Czech Republic.

Stefan Hüttelmaier (S)

Institute of Molecular Medicine, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany.

Mike Schutkowski (M)

Charles Tanford Protein Center, Department of Enzymology, Institute of Biochemistry and Biotechnology, Martin-Luther-University of Halle-Wittenberg, Halle (Saale), Germany.

Wolfgang Sippl (W)

Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, Halle (Saale), Germany.

Classifications MeSH