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Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists.
Kosar M, Sarott RC, Sykes DA, Viray AEG, Vitale RM, Tomašević N, Li X, Ganzoni RLZ, Kicin B, Reichert L, Patej KJ, Gómez-Bouzó U, Guba W, McCormick PJ, Hua T, Gruber CW, Veprintsev DB, Frank JA, Grether U, Carreira EM. Kosar M, et al. Among authors: veprintsev db. ACS Cent Sci. 2024 Mar 11;10(5):956-968. doi: 10.1021/acscentsci.3c01461. eCollection 2024 May 22. ACS Cent Sci. 2024. PMID: 38799662 Free PMC article.
ThermoBRET: A Ligand-Engagement Nanoscale Thermostability Assay Applied to GPCRs.
Hoare BL, Tippett DN, Kaur A, Cullum SA, Miljuš T, Koers EJ, Harwood CR, Dijon N, Holliday ND, Sykes DA, Veprintsev DB. Hoare BL, et al. Among authors: veprintsev db. Chembiochem. 2024 Jan 15;25(2):e202300459. doi: 10.1002/cbic.202300459. Epub 2023 Nov 28. Chembiochem. 2024. PMID: 37872746
Platform Reagents Enable Synthesis of Ligand-Directed Covalent Probes: Study of Cannabinoid Receptor 2 in Live Cells.
Kosar M, Sykes DA, Viray AEG, Vitale RM, Sarott RC, Ganzoni RL, Onion D, Tobias JM, Leippe P, Ullmer C, Zirwes EA, Guba W, Grether U, Frank JA, Veprintsev DB, Carreira EM. Kosar M, et al. Among authors: veprintsev db. J Am Chem Soc. 2023 Jul 19;145(28):15094-15108. doi: 10.1021/jacs.2c13629. Epub 2023 Jul 4. J Am Chem Soc. 2023. PMID: 37401816
Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor.
Jiménez-Rosés M, Morgan BA, Jimenez Sigstad M, Tran TDZ, Srivastava R, Bunsuz A, Borrega-Román L, Hompluem P, Cullum SA, Harwood CR, Koers EJ, Sykes DA, Styles IB, Veprintsev DB. Jiménez-Rosés M, et al. Among authors: veprintsev db. Pharmacol Res Perspect. 2022 Oct;10(5):e00994. doi: 10.1002/prp2.994. Pharmacol Res Perspect. 2022. PMID: 36029004 Free PMC article.
Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe.
Gazzi T, Brennecke B, Atz K, Korn C, Sykes D, Forn-Cuni G, Pfaff P, Sarott RC, Westphal MV, Mostinski Y, Mach L, Wasinska-Kalwa M, Weise M, Hoare BL, Miljuš T, Mexi M, Roth N, Koers EJ, Guba W, Alker A, Rufer AC, Kusznir EA, Huber S, Raposo C, Zirwes EA, Osterwald A, Pavlovic A, Moes S, Beck J, Nettekoven M, Benito-Cuesta I, Grande T, Drawnel F, Widmer G, Holzer D, van der Wel T, Mandhair H, Honer M, Fingerle J, Scheffel J, Broichhagen J, Gawrisch K, Romero J, Hillard CJ, Varga ZV, van der Stelt M, Pacher P, Gertsch J, Ullmer C, McCormick PJ, Oddi S, Spaink HP, Maccarrone M, Veprintsev DB, Carreira EM, Grether U, Nazaré M. Gazzi T, et al. Among authors: veprintsev db. Chem Sci. 2022 Apr 1;13(19):5539-5545. doi: 10.1039/d1sc06659e. eCollection 2022 May 18. Chem Sci. 2022. PMID: 35694350 Free PMC article.
84 results