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2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
Johansson L, Fotsch C, Bartberger MD, Castro VM, Chen M, Emery M, Gustafsson S, Hale C, Hickman D, Homan E, Jordan SR, Komorowski R, Li A, McRae K, Moniz G, Matsumoto G, Orihuela C, Palm G, Veniant M, Wang M, Williams M, Zhang J. Johansson L, et al. Among authors: komorowski r. J Med Chem. 2008 May 22;51(10):2933-43. doi: 10.1021/jm701551j. Epub 2008 Apr 18. J Med Chem. 2008. PMID: 18419108
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Fotsch C, Bartberger MD, Bercot EA, Chen M, Cupples R, Emery M, Fretland J, Guram A, Hale C, Han N, Hickman D, Hungate RW, Hayashi M, Komorowski R, Liu Q, Matsumoto G, St Jean DJ Jr, Ursu S, Véniant M, Xu G, Ye Q, Yuan C, Zhang J, Zhang X, Tu H, Wang M. Fotsch C, et al. Among authors: komorowski r. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Véniant MM, Hale C, Hungate RW, Gahm K, Emery MG, Jona J, Joseph S, Adams J, Hague A, Moniz G, Zhang J, Bartberger MD, Li V, Syed R, Jordan S, Komorowski R, Chen MM, Cupples R, Kim KW, St Jean DJ Jr, Johansson L, Henriksson MA, Williams M, Vallgårda J, Fotsch C, Wang M. Véniant MM, et al. Among authors: komorowski r. J Med Chem. 2010 Jun 10;53(11):4481-7. doi: 10.1021/jm100242d. J Med Chem. 2010. PMID: 20465278
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase.
Bourbeau MP, Siegmund A, Allen JG, Shu H, Fotsch C, Bartberger MD, Kim KW, Komorowski R, Graham M, Busby J, Wang M, Meyer J, Xu Y, Salyers K, Fielden M, Véniant MM, Gu W. Bourbeau MP, et al. Among authors: komorowski r. J Med Chem. 2013 Dec 27;56(24):10132-41. doi: 10.1021/jm401601s. Epub 2013 Dec 11. J Med Chem. 2013. PMID: 24294923
Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors.
Lloyd DJ, St Jean DJ Jr, Kurzeja RJ, Wahl RC, Michelsen K, Cupples R, Chen M, Wu J, Sivits G, Helmering J, Komorowski R, Ashton KS, Pennington LD, Fotsch C, Vazir M, Chen K, Chmait S, Zhang J, Liu L, Norman MH, Andrews KL, Bartberger MD, Van G, Galbreath EJ, Vonderfecht SL, Wang M, Jordan SR, Véniant MM, Hale C. Lloyd DJ, et al. Among authors: komorowski r. Nature. 2013 Dec 19;504(7480):437-40. doi: 10.1038/nature12724. Epub 2013 Nov 13. Nature. 2013. PMID: 24226772
Long-acting MIC-1/GDF15 molecules to treat obesity: Evidence from mice to monkeys.
Xiong Y, Walker K, Min X, Hale C, Tran T, Komorowski R, Yang J, Davda J, Nuanmanee N, Kemp D, Wang X, Liu H, Miller S, Lee KJ, Wang Z, Véniant MM. Xiong Y, et al. Among authors: komorowski r. Sci Transl Med. 2017 Oct 18;9(412):eaan8732. doi: 10.1126/scitranslmed.aan8732. Sci Transl Med. 2017. PMID: 29046435
247 results