Identification and validation of a selective small molecule inhibitor targeting the diacylglycerol acyltransferase 2 activity = 디아실글리세롤 아실트랜스퍼라제 선택적 억제물질 발굴 및 검증

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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
Author(s)
Mun-Ock KimSu Ui LeeHyun Jun Lee; Kwangman Choi; Hyeongki Kim; Sangku Lee; Soo Jin Oh; Sunhong Kim; Jong Soon Kang; Hyun Sun Lee; Y S Kwak; Sungchan Cho
Bibliographic Citation
Biological & Pharmaceutical Bulletin, vol. 36, no. 7, pp. 1167-1173
Publication Year
2013
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.
Keyword
Diacylglycerol acyltransferase 2IsatinMetabolic diseaseSmall molecule inhibitorTriacylglycerol
ISSN
0918-6158
Publisher
Pharmaceutical Soc Japan
DOI
http://dx.doi.org/10.1248/bpb.b13-00152
Type
Article
Appears in Collections:
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
Ochang Branch Institute > Nucleic Acid Therapeutics Research Center > 1. Journal Articles
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