Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Identification and Validation of a Selective Small Molecule Inhibitor Targeting the Diacylglycerol Acyltransferase 2 Activity
Mun Ock Kim, Su Ui Lee, Hyun-Jun Lee, Kwangman Choi, Hyeongki Kim, Sangku Lee, Soo Jin Oh, Sunhong Kim, Jong Soon Kang, Hyun Sun Lee, Young-Shin Kwak, Sungchan Cho
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Keywords: metabolic disease, triacylglycerol, diacylglycerol acyltransferase 2, small molecule inhibitor, isatin
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2013 Volume 36 Issue 7 Pages 1167-1173

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J-STAGE : bpb 37 4 pp.707-707
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Abstract

Diacylglycerol acyltransferase 2 (DGAT2) is one of two distinct DGAT enzymes that catalyze the last step in triacylglycerol (TG) synthesis. Findings from previous studies suggest that inhibition of DGAT2 is a promising strategy for the treatment of hepatic steatosis and insulin resistance. Here, we identified compound 122 as a potent and selective inhibitor of human DGAT2, which appeared to act competitively against oleoyl-CoA in vitro. The selective inhibition of DGAT2 was also confirmed by the reductions in enzymatic activity and de novo TG synthesis in DGAT2-overexpressing HEK293 cells and hepatic cells HepG2. Compound 122, as a newly identified inhibitor of DGAT2, will be useful for the research on DGAT2-related lipid metabolism as well as the development of therapeutic drug for several metabolic diseases.

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© 2013 The Pharmaceutical Society of Japan
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