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Title 

Identification and validation of a selective small molecule inhibitor targeting the diacylglycerol acyltransferase 2 activity

 

디아실글리세롤 아실트랜스퍼라제 선택적 억제물질 발굴 및 검증

Authors 

Mun-Ock KimSu Ui LeeHyun Jun LeeKwangman ChoiHyeongki KimSangku LeeSoo Jin OhSunhong KimJong Soon KangHyun Sun LeeY S KwakSungchan Cho

Publisher 

Pharmaceutical Society of Japan

Issue Date 

2013

Citation 

Biological & Pharmaceutical Bulletin, vol. 36, no. 7, pp. 1167-1173

Keywords 

Diacylglycerol acyltransferase 2IsatinMetabolic diseaseSmall molecule inhibitorTriacylglycerol

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.

ISSN 

0918-6158

Link 

http://dx.doi.org/10.1248/bpb.b13-00152

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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