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Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB1R).
Mach L, Omran A, Bouma J, Radetzki S, Sykes DA, Guba W, Li X, Höffelmeyer C, Hentsch A, Gazzi T, Mostinski Y, Wasinska-Kalwa M, de Molnier F, van der Horst C, von Kries JP, Vendrell M, Hua T, Veprintsev DB, Heitman LH, Grether U, Nazare M. Mach L, et al. Among authors: sykes da. J Med Chem. 2024 Jul 25;67(14):11841-11867. doi: 10.1021/acs.jmedchem.4c00465. Epub 2024 Jul 11. J Med Chem. 2024. PMID: 38990855 Free PMC article.
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: sykes da. 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
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: sykes da. 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.
Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.
Aebi J, Atz K, Ametamey SM, Benz J, Blaising J, Butini S, Campiani G, Carreira EM, Collin L, De Lago E, Gazzi T, Gertsch J, Gobbi L, Guba W, Fernández-Ruiz J, Fingerle J, Haider A, He Y, Heitman LH, Honer M, Hunziker D, Kuhn B, Maccarrone M, Märki HP, Martin RE, Mohr P, Mu L, Nazaré M, Nippa DF, Oddi S, O'Hara F, Pacher P, Romero J, Röver S, Rufer AC, Schibli R, Schneider G, Stepan AF, Sykes DA, Ullmer C, Van der Stelt M, Veprintsev DB, Wittwer MB, Grether U. Aebi J, et al. Among authors: sykes da. Chimia (Aarau). 2024 Aug 21;78(7-8):499-512. doi: 10.2533/chimia.2024.499. Chimia (Aarau). 2024. PMID: 39221845 Free article.
Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization.
Butini S, Grether U, Jung KM, Ligresti A, Allarà M, Postmus AGJ, Maramai S, Brogi S, Papa A, Carullo G, Sykes D, Veprintsev D, Federico S, Grillo A, Di Guglielmo B, Ramunno A, Stevens AF, Heer D, Lamponi S, Gemma S, Benz J, Di Marzo V, van der Stelt M, Piomelli D, Campiani G. Butini S, et al. J Med Chem. 2024 Feb 8;67(3):1758-1782. doi: 10.1021/acs.jmedchem.3c01278. Epub 2024 Jan 19. J Med Chem. 2024. PMID: 38241614
Visualization of membrane localization and the functional state of CB2R pools using matched agonist and inverse agonist probe pairs.
Wąsińska-Kałwa M, Omran A, Mach L, Scipioni L, Bouma J, Li X, Radetzki S, Mostinski Y, Schippers M, Gazzi T, van der Horst C, Brennecke B, Hanske A, Kolomeets Y, Guba W, Sykes D, von Kries JP, Broichhagen J, Hua T, Veprintsev D, Heitman LH, Oddi S, Maccarrone M, Grether U, Nazare M. Wąsińska-Kałwa M, et al. Chem Sci. 2024 Oct 3;15(44):18443-54. doi: 10.1039/d4sc00402g. Online ahead of print. Chem Sci. 2024. PMID: 39430942 Free PMC article.
67 results