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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: fingerle j. Chimia (Aarau). 2024 Aug 21;78(7-8):499-512. doi: 10.2533/chimia.2024.499. Chimia (Aarau). 2024. PMID: 39221845 Free article.
A Highly Potent, Orally Bioavailable Pyrazole-Derived Cannabinoid CB2 Receptor- Selective Full Agonist for In Vivo Studies.
Chicca A, Bátora D, Ullmer C, Caruso A, Grüner S, Fingerle J, Hartung T, Degen R, Müller M, Grether U, Pacher P, Gertsch J. Chicca A, et al. Among authors: fingerle j. ACS Pharmacol Transl Sci. 2024 Jul 9;7(8):2424-2438. doi: 10.1021/acsptsci.4c00269. eCollection 2024 Aug 9. ACS Pharmacol Transl Sci. 2024. PMID: 39144568 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: fingerle j. Front Pharmacol. 2024 Jul 12;15:1426446. doi: 10.3389/fphar.2024.1426446. eCollection 2024. Front Pharmacol. 2024. PMID: 39070793 Free PMC article.
A highly potent, orally bioavailable pyrazole-derived cannabinoid CB2 receptor-selective full agonist for in vivo studies.
Chicca A, Batora D, Ullmer C, Caruso A, Fingerle J, Hartung T, Degen R, Müller M, Grether U, Pacher P, Gertsch J. Chicca A, et al. Among authors: fingerle j. bioRxiv [Preprint]. 2024 Apr 29:2024.04.26.591311. doi: 10.1101/2024.04.26.591311. bioRxiv. 2024. Update in: ACS Pharmacol Transl Sci. 2024 Jul 09;7(8):2424-2438. doi: 10.1021/acsptsci.4c00269. PMID: 38903103 Free PMC article. Updated. Preprint.
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: fingerle j. 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.
Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.
Sarott RC, Westphal MV, Pfaff P, Korn C, Sykes DA, Gazzi T, Brennecke B, Atz K, Weise M, Mostinski Y, Hompluem P, Koers E, Miljuš T, Roth NJ, Asmelash H, Vong MC, Piovesan J, Guba W, Rufer AC, Kusznir EA, Huber S, Raposo C, Zirwes EA, Osterwald A, Pavlovic A, Moes S, Beck J, Benito-Cuesta I, Grande T, Ruiz de Martı N Esteban S, Yeliseev A, Drawnel F, Widmer G, Holzer D, van der Wel T, Mandhair H, Yuan CY, Drobyski WR, Saroz Y, Grimsey N, Honer M, Fingerle J, Gawrisch K, Romero J, Hillard CJ, Varga ZV, van der Stelt M, Pacher P, Gertsch J, McCormick PJ, Ullmer C, Oddi S, Maccarrone M, Veprintsev DB, Nazaré M, Grether U, Carreira EM. Sarott RC, et al. Among authors: fingerle j. J Am Chem Soc. 2020 Oct 7;142(40):16953-16964. doi: 10.1021/jacs.0c05587. Epub 2020 Sep 29. J Am Chem Soc. 2020. PMID: 32902974
Structure-Activity Relationship Studies of Pyridine-Based Ligands and Identification of a Fluorinated Derivative for Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors.
Haider A, Kretz J, Gobbi L, Ahmed H, Atz K, Bürkler M, Bartelmus C, Fingerle J, Guba W, Ullmer C, Honer M, Knuesel I, Weber M, Brink A, Herde AM, Keller C, Schibli R, Mu L, Grether U, Ametamey SM. Haider A, et al. Among authors: fingerle j. J Med Chem. 2019 Dec 26;62(24):11165-11181. doi: 10.1021/acs.jmedchem.9b01280. Epub 2019 Dec 5. J Med Chem. 2019. PMID: 31751140
Selective Cannabinoid 2 Receptor Agonists as Potential Therapeutic Drugs for the Treatment of Endotoxin-Induced Uveitis.
Porter RF, Szczesniak AM, Toguri JT, Gebremeskel S, Johnston B, Lehmann C, Fingerle J, Rothenhäusler B, Perret C, Rogers-Evans M, Kimbara A, Nettekoven M, Guba W, Grether U, Ullmer C, Kelly MEM. Porter RF, et al. Among authors: fingerle j. Molecules. 2019 Sep 13;24(18):3338. doi: 10.3390/molecules24183338. Molecules. 2019. PMID: 31540271 Free PMC article.
63 results