Identification and Validation of a Selective Small Molecule Inhibitor Targeting the Diacylglycerol Acyltransferase 2 Activity

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  • Kim Mun Ock
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Lee Su Ui
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Lee Hyun-Jun
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Choi Kwangman
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Kim Hyeongki
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Lee Sangku
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Oh Soo Jin
    Bio-Evaluation Center, Korea Research Institute of Bioscience and Biotechnology
  • Kim Sunhong
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology Department of Biomolecular Science, University of Science and Technology
  • Kang Jong Soon
    Bio-Evaluation Center, Korea Research Institute of Bioscience and Biotechnology
  • Lee Hyun Sun
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology
  • Kwak Young-Shin
    College of Pharmacy, Korea University
  • Cho Sungchan
    Targeted Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology Department of Biomolecular Science, University of Science and Technology

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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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