Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors

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• 作者：Jason E. Imbriglio ; Dong-Ming Shen ; Rui Liang ; Ken Marby ; Ming You ; Hye Won Youm ; Zhe Feng ; Clare London ; Yusheng Xiong ; Jim Tata ; Andreas Verras ; Margarita Garcia-Calvo ; Xuelei Song ; George H. Addona ; Dave G. McLaren ; Timothy He ; Beth Murphy ; Dan E. Metzger ; Gino Salituro ; Diana Deckman ; Qing Chen ; Xiaoling Jin ; Steven J. Stout ; Sheng-Ping Wang ; Larissa Wilsie ; Oksana Palyha ; Seongah Han ; Brian K. Hubbard ; Stephen F. Previs ; Shirly Pinto ; Andrew Taggart
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：December 10, 2015
• 年：2015
• 卷：58
• 期：23
• 页码：9345-9353
• 全文大小：407K
• ISSN：1520-4804

文摘

DGAT2 plays a critical role in hepatic triglyceride production, and data suggests that inhibition of DGAT2 could prove to be beneficial in treating a number of disease states. This article documents the discovery and optimization of a selective small molecule inhibitor of DGAT2 as well as pharmacological proof of biology in a mouse model of triglyceride production.