A novel and selective fluorescent ligand for the study of adenosine A
PSB603
adenosine A2B receptor
antagonist
fluorescent ligand
ligand‐binding
macrophages
Journal
Pharmacology research & perspectives
ISSN: 2052-1707
Titre abrégé: Pharmacol Res Perspect
Pays: United States
ID NLM: 101626369
Informations de publication
Date de publication:
Aug 2024
Aug 2024
Historique:
revised:
25
04
2024
received:
16
02
2024
accepted:
27
05
2024
medline:
20
7
2024
pubmed:
20
7
2024
entrez:
20
7
2024
Statut:
ppublish
Résumé
Fluorescent ligands have proved to be powerful tools in the study of G protein-coupled receptors in living cells. Here we have characterized a new fluorescent ligand PSB603-BY630 that has high selectivity for the human adenosine A
Substances chimiques
Receptor, Adenosine A2B
0
Ligands
0
Fluorescent Dyes
0
Adenosine A2 Receptor Antagonists
0
Adenosine A2 Receptor Agonists
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
e1223Subventions
Organisme : Medical Research Council
ID : MR/W016176/1
Pays : United Kingdom
Organisme : Cancer Research UK
ID : C50808/A24952
Pays : United Kingdom
Organisme : Biotechnology and Biological Sciences Research Council
ID : BB/T0083690/1
Pays : United Kingdom
Informations de copyright
© 2024 The Author(s). Pharmacology Research & Perspectives published by British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics and John Wiley & Sons Ltd.
Références
Fredholm BB, IJzerman AP, Jacobson KA, Linden J, Müller CE. International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors‐an update. Pharmacol Rev. 2011;63(1):1‐34. doi:10.1124/pr.110.003285
Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of adenosine receptors: the state of the art. Physiol Rev. 2018;98(3):1591‐1625.
Müller CE, Jacobson KA. Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011;1808(5):1290‐1308.
Goulding J, May LT, Hill SJ. Characterisation of endogenous A2A and A2B receptor‐mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: evidence for an allosteric mechanism of action for the A2B‐selective antagonist PSB 603. Biochem Pharmacol. 2018;147:55‐66.
Hinz S, Lacher SK, Seibt BF, Müller CE. BAY60‐6583 acts as a partial agonist at adenosine A2B receptors. J Pharmacol Exp Ther. 2014;349(3):427‐436.
Gao ZG, Inoue A, Jacobson KA. On the G protein‐coupling selectivity of the native A2B adenosine receptor. Biochem Pharmacol. 2018;151:201‐213.
Linden J, Thai T, Figler H, Jin X, Robeva AS. Characterization of human a(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC‐1 mast cells. Mol Pharmacol. 1999;56(4):705‐713.
Voss JH, Mahardhika AB, Inoue A, Müller CE. Agonist‐dependent coupling of the promiscuous adenosine A2B receptor to Gα protein subunits. ACS Pharmacol Transl Sci. 2022;5(5):373‐386.
Jaakola VP, Griffith MT, Hanson MA, et al. The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science. 2008;322(5905):1211‐1217.
Lebon G, Warne T, Edwards PC, et al. Agonist‐bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature. 2011;474(7352):521‐525.
Xu F, Wu H, Katritch V, et al. Structure of an agonist‐bound human A2A adenosine receptor. Science. 2011;332(6027):322‐327.
García‐Nafría J, Lee Y, Bai X, Carpenter B, Tate CG. Cryo‐EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein. elife. 2018;4(7):e35946.
Thimm D, Schiedel AC, Sherbiny FF, et al. Ligand‐specific binding and activation of the human adenosine a(2B) receptor. Biochemistry. 2013;52(4):726‐740.
Chen Y, Zhang J, Weng Y, et al. Cryo‐EM structure of the human adenosine A2B receptor‐Gs signaling complex. Sci Adv. 2022;8(51):eadd3709.
Ohta A, Gorelik E, Prasad SJ, et al. A2A adenosine receptor protects tumors from antitumor T cells. Proc Natl Acad Sci USA. 2006;103(35):13132‐13137.
Ohta A. A metabolic immune checkpoint: adenosine inTumor microenvironment. Front Immunol. 2016;7:109.
Inoue Y, Yoshimura K, Kurabe N, et al. Prognostic impact of CD73 and A2A adenosine receptor expression in non‐small‐cell lung cancer. Oncotarget. 2017;8:8738‐8751.
Zhang C, Wang K, Wang H. Adenosine in cancer immunotherapy: taking off on a new plane. Biochim Biophys Acta Rev Cancer. 2023;1878(6):189005.
Yu F, Zhu C, Xie Q, Wang Y. Adenosine A2A receptor antagonists for cancer immunotherapy. J Med Chem. 2020;63(21):12196‐12212.
Evans JV, Suman S, Goruganthu MUL, et al. Improving combination therapies: targeting A2B‐adenosine receptor to modulate metabolic tumor microenvironment and immunosuppression. J Natl Cancer Inst. 2023;115(11):1404‐1419.
Strickland LN, Faraoni EY, Ruan W, Yuan X, Eltzschig HK, Bailey‐Lundberg JM. The resurgence of the Adora2b receptor as an immunotherapeutic target in pancreatic cancer. Front Immunol. 2023;28(14):1163585.
Dutta S, Ganguly A, Chatterjee K, Spada S, Mukherjee S. Targets of immune escape mechanisms in cancer: basis for development and evolution of cancer immune checkpoint inhibitors. Biology (Basel). 2023;12(2):218.
Ludwig N, Yerneni SS, Azambuja JH, et al. Tumor‐derived exosomes promote angiogenesis via adenosine A2B receptor signaling. Angiogenesis. 2020;23(4):599‐610.
Hill SJ, Kilpatrick LE. Kinetic analysis of fluorescent ligand binding to cell surface receptors: insights into conformational changes and allosterism in living cells. Br J Pharmacol. 2023.
Goulding J, Kondrashov A, Mistry SJ, et al. The use of fluorescence correlation spectroscopy to monitor cell surface β2‐adrenoceptors at low expression levels in human embryonic stem cell‐derived cardiomyocytes and fibroblasts. FASEB J. 2021;35(4):e21398.
Lay CS, Isidro‐Llobet A, Kilpatrick LE, Craggs PD, Hill SJ. Characterisation of IL‐23 receptor antagonists and disease relevant mutants using fluorescent probes. Nat Commun. 2023;14(1):2882.
White CW, Caspar B, Vanyai HK, Pfleger KDG, Hill SJ. CRISPR‐mediated protein tagging with Nanoluciferase to investigate native chemokine receptor function and conformational changes. Cell Chem Biol. 2020;27(5):499‐510.e7.
Comeo E, Kindon ND, Soave M, et al. Subtype‐selective fluorescent ligands as pharmacological research tools for the human adenosine A2A receptor. J Med Chem. 2020;63(5):2656‐2672.
Stoddart LA, Kindon ND, Otun O, et al. Ligand‐directed covalent labelling of a GPCR with a fluorescent tag in live cells. Commun Biol. 2020;3(1):722.
Neustadt BR, Hao J, Lindo N, et al. Potent, selective, and orally active adenosine A2Areceptor antagonists: Arylpiperazine derivatives of Pyrazolo[4,3‐e]‐1,2,4‐Triazolo[1,5‐c]pyrimidines. Bioorg Med Chem Lett. 2007;17(5):1376‐1380.
Köse M, Gollos S, Karcz T, et al. Fluorescent‐labeled selective adenosine A2B receptor antagonist enables competition binding assay by flow cytometry. J Med Chem. 2018;61(10):4301‐4316.
Borrmann T, Hinz S, Bertarelli DC, et al. 1‐alkyl‐8‐(piperazine‐1‐sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. J Med Chem. 2009;52(13):3994‐4006.
Vernall AJ, Stoddart LA, Briddon SJ, Hill SJ, Kellam B. Highly potent and selective fluorescent antagonists of the human adenosine a₃ receptor based on the 1,2,4‐triazolo[4,3‐a]quinoxalin‐1‐one scaffold. J Med Chem. 2012;55:1771‐1782.
Comeo E, Trinh P, Nguyen AT, et al. Development and application of subtype‐selective fluorescent antagonists for the study of the human adenosine A1Receptor in living cells. J Med Chem. 2021;64(10):6670‐6695.
Fan F, Binkowski BF, Butler BL, Stecha PF, Lewis MK, Wood KV. Novel genetically encoded biosensors using firefly luciferase. ACS Chem Biol. 2008;3:346‐351.
Stoddart LA, Johnstone EKM, Wheal AJ, et al. Application of BRET to monitor ligand binding to GPCRs. Nat Methods. 2015;12(7):661‐663.
Cooper SL, Wragg ES, Pannucci P, Soave M, Hill SJ, Woolard J. Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation. FASEB J. 2022;36(4):e22214.
Balaji J, Ryan TA. Single‐vesicle imaging reveals that synaptic vesicle exocytosis and endocytosis are coupled by a single stochastic mode. Proc Natl Acad Sci USA. 2007;104:20576‐20581.
Harding SD, Sharman JL, Faccenda E, et al. The IUPHAR/BPS guide to pharmacology in 2019: updates and expansion to encompass the new guide to immunopharmacology. Nucleic Acids Res. 2018; 46:D1091‐D1106.
Alexander SPH, Christopoulos A, Davenport AP, et al. The concise guide to pharmacology 2019/20: g protein‐coupled receptors. Br J Pharmacol. 2019;176(1):S21‐S141.
Baker JG, Middleton R, Adams L, et al. Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands. Br J Pharmacol. 2010;159(4):772‐786.
Kok ZY, Stoddart LA, Mistry SJ, et al. Optimization of peptide linker‐based fluorescent ligands for the histamine H1 receptor. J Med Chem. 2022;65(12):8258‐8288.
Jiang J, Seel CJ, Temirak A, et al. A2B adenosine receptor antagonists with Picomolar potency. J Med Chem. 2019;62(8):4032‐4055.
Trincavelli ML, Marroni M, Tuscano D, et al. Regulation of A2B adenosine receptor functioning by tumour necrosis factor a in human astroglial cells. J Neurochem. 2004;91(5):1180‐1190.
Ongini E, Dionisotti S, Gessi S, Irenius E, Fredholm BB. Comparison of CGS15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors. Naunyn Schmiedeberg's Arch Pharmacol. 1999;359:7‐10.
Moresco RM, Todde S, Belloli S, et al. In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416. Eur J Nucl Med Mol Imaging. 2005;32(4):405‐413.