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Page 1
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
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
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
Pharmacological targeting of glucagon and glucagon-like peptide 1 receptors has different effects on energy state and glucose homeostasis in diet-induced obese mice.
Gu W, Lloyd DJ, Chinookswong N, Komorowski R, Sivits G Jr, Graham M, Winters KA, Yan H, Boros LG, Lindberg RA, Véniant MM. Gu W, et al. Among authors: komorowski r. J Pharmacol Exp Ther. 2011 Jul;338(1):70-81. doi: 10.1124/jpet.111.179986. Epub 2011 Apr 6. J Pharmacol Exp Ther. 2011. PMID: 21471191
Long-term inhibition of the glucagon receptor with a monoclonal antibody in mice causes sustained improvement in glycemic control, with reversible alpha-cell hyperplasia and hyperglucagonemia.
Gu W, Yan H, Winters KA, Komorowski R, Vonderfecht S, Atangan L, Sivits G, Hill D, Yang J, Bi V, Shen Y, Hu S, Boone T, Lindberg RA, Véniant MM. Gu W, et al. Among authors: komorowski r. J Pharmacol Exp Ther. 2009 Dec;331(3):871-81. doi: 10.1124/jpet.109.157685. Epub 2009 Aug 31. J Pharmacol Exp Ther. 2009. PMID: 19720878
247 results