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Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.
Richter HG, Benson GM, Bleicher KH, Blum D, Chaput E, Clemann N, Feng S, Gardes C, Grether U, Hartman P, Kuhn B, Martin RE, Plancher JM, Rudolph MG, Schuler F, Taylor S. Richter HG, et al. Among authors: rudolph mg. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1134-40. doi: 10.1016/j.bmcl.2010.12.123. Epub 2010 Dec 31. Bioorg Med Chem Lett. 2011. PMID: 21269824
A Real-World Perspective on Molecular Design.
Kuhn B, Guba W, Hert J, Banner D, Bissantz C, Ceccarelli S, Haap W, Körner M, Kuglstatter A, Lerner C, Mattei P, Neidhart W, Pinard E, Rudolph MG, Schulz-Gasch T, Woltering T, Stahl M. Kuhn B, et al. Among authors: rudolph mg. J Med Chem. 2016 May 12;59(9):4087-102. doi: 10.1021/acs.jmedchem.5b01875. Epub 2016 Feb 24. J Med Chem. 2016. PMID: 26878596
Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors.
Kühne H, Obst-Sander U, Kuhn B, Conte A, Ceccarelli SM, Neidhart W, Rudolph MG, Ottaviani G, Gasser R, So SS, Li S, Zhang X, Gao L, Myers M. Kühne H, et al. Among authors: rudolph mg. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5092-5097. doi: 10.1016/j.bmcl.2016.08.071. Epub 2016 Aug 22. Bioorg Med Chem Lett. 2016. PMID: 27658368
Ligand channel in pharmacologically stabilized rhodopsin.
Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP. Mattle D, et al. Among authors: rudolph mg. Proc Natl Acad Sci U S A. 2018 Apr 3;115(14):3640-3645. doi: 10.1073/pnas.1718084115. Epub 2018 Mar 19. Proc Natl Acad Sci U S A. 2018. PMID: 29555765 Free PMC article.
Discovery of Orally Available and Brain Penetrant AEP Inhibitors.
Krummenacher D, He W, Kuhn B, Schnider C, Beurier A, Brom V, Sivasothy T, Marty C, Tosstorff A, Hewings DS, Mesch S, Pinard E, Brändlin M, Hochstrasser R, Westwood P, Rothe J, Kronenberger A, Morandi F, Gutbier S, Schuler A, Heer D, Gloria LE, Joedicke L, Rudolph MG, Müller L, Grüninger F, Baumann K, Kaniyappan S, Manevski N, Bartels B. Krummenacher D, et al. Among authors: rudolph mg. J Med Chem. 2023 Dec 28;66(24):17026-17043. doi: 10.1021/acs.jmedchem.3c01804. Epub 2023 Dec 13. J Med Chem. 2023. PMID: 38090813
Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist.
Feng S, Yang M, Zhang Z, Wang Z, Hong D, Richter H, Benson GM, Bleicher K, Grether U, Martin RE, Plancher JM, Kuhn B, Rudolph MG, Chen L. Feng S, et al. Among authors: rudolph mg. Bioorg Med Chem Lett. 2009 May 1;19(9):2595-8. doi: 10.1016/j.bmcl.2009.03.008. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19328688
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