Journal
BIOLOGICAL & PHARMACEUTICAL BULLETIN
Volume 36, Issue 7, Pages 1167-1173Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.b13-00152
Keywords
metabolic disease; triacylglycerol; diacylglycerol acyltransferase 2; small molecule inhibitor; isatin
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Funding
- Basic Science Research Program through the National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2012R1A1A2003182]
- International Science and Business Belt Program through the Ministry of Science, ICT and Future Planning [2012K001574]
- KRIBB Research Initiative Program
- National Research Foundation of Korea [2012R1A1A2003182] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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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