Discovery of PF-04620110, a potent, selective, and orally bioavailable inhibitor of DGAT-1

…, J Litchfield, DW Piotrowski, MJ Munchhof…

Index: Dow, Robert L.; Li, Jian-Cheng; Pence, Michael P.; Gibbs, E. Michael; Laperle, Jennifer L.; Litchfield, John; Piotrowski, David W.; Munchhof, Michael J.; Manion, Tara B.; Zavadoski, William J.; Walker, Gregory S.; McPherson, R. Kirk; Tapley, Susan; Sugarman, Eliot; Guzman-Perez, Angel; Dasilva-Jardine, Paul ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 5 p. 407 - 412

Full Text: HTML

Citation Number: 38

Abstract

Acyl-CoA: diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides. DGAT-1 knockout mice have been shown to be resistant to diet-induced obesity and have increased insulin sensitivity. Thus, inhibition of DGAT-1 may represent an attractive target for the treatment of obesity or type II diabetes. Herein, we report the discovery and characterization of a potent and selective DGAT-1 inhibitor PF- ...