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Page 1
Novel Macrocyclic NLRP3 Inhibitors.
Mesch S, Shannon J, Miller D, MacLeod A, Bouché L, Johnston HJ, Matthews K, Paehler A, Best S, Guba W, Alanine T, Halai R, Charge L, Garside S, Thom S, Incerti-Pradillos C, McPherson C, Carrillo J, St-Gallay S, Rigo P, Schlicht S, Hendrick AG, Lerner C, Piali L, Blaising J, Mracsko EZ, Jaeschke G, Cooper MA. Mesch S, et al. Among authors: guba w. J Med Chem. 2024 Nov 25. doi: 10.1021/acs.jmedchem.4c01376. Online ahead of print. J Med Chem. 2024. PMID: 39585325
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. Among authors: guba w. 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.
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: guba w. Chimia (Aarau). 2024 Aug 21;78(7-8):499-512. doi: 10.2533/chimia.2024.499. Chimia (Aarau). 2024. PMID: 39221845 Free article.
RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models.
Grether U, Foxton RH, Gruener S, Korn C, Kimbara A, Osterwald A, Zirwes E, Uhles S, Thoele J, Colé N, Rogers-Evans M, Röver S, Nettekoven M, Martin RE, Adam JM, Fingerle J, Bissantz C, Guba W, Alker A, Szczesniak AM, Porter RF, Toguri TJ, Revelant F, Poirier A, Perret C, Winther L, Caruso A, Fezza F, Maccarrone M, Kelly MEM, Fauser S, Ullmer C. Grether U, et al. Among authors: guba w. Front Pharmacol. 2024 Jul 12;15:1426446. doi: 10.3389/fphar.2024.1426446. eCollection 2024. Front Pharmacol. 2024. PMID: 39070793 Free PMC article.
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: guba w. 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.
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: guba w. 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.
59 results