Identification and Validation of a Selective Small Molecule Inhibitor Targeting the Diacylglycerol Acyltransferase 2 Activity
- Authors
- Kim, Mun Ock; Lee, Su Ui; Lee, Hyun-Jun; Choi, Kwangman; Kim, Hyeongki; Lee, Sangku; Oh, Soo Jin; Kim, Sunhong; Kang, Jong Soon; Lee, Hyun Sun; Kwak, Young-Shin; Cho, Sungchan
- Issue Date
- 7월-2013
- Publisher
- PHARMACEUTICAL SOC JAPAN
- Keywords
- metabolic disease; triacylglycerol; diacylglycerol acyltransferase 2; small molecule inhibitor; isatin
- Citation
- BIOLOGICAL & PHARMACEUTICAL BULLETIN, v.36, no.7, pp.1167 - 1173
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOLOGICAL & PHARMACEUTICAL BULLETIN
- Volume
- 36
- Number
- 7
- Start Page
- 1167
- End Page
- 1173
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/102758
- DOI
- 10.1248/bpb.b13-00152
- ISSN
- 0918-6158
- 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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Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
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