Therapeutic Strategies for Metabolic Diseases: Small-Molecule Diacylglycerol Acyltransferase (DGAT) Inhibitors

Ravi Naik, Brice W. Obiang-Obounou, Minkyoung Kim, Yongseok Choi, Hyun Sun Lee, Kyeong Lee

Research output: Contribution to journalReview articlepeer-review

32 Citations (Scopus)


Metabolic diseases such as atherogenic dyslipidemia, hepatic steatosis, obesity, and type II diabetes are emerging as major global health problems. Acyl-CoA:diacylglycerol acyltransferase (DGAT) is responsible for catalyzing the final reaction in the glycerol phosphate pathway of triglycerol synthesis. It has two isoforms, DGAT-1 and DGAT-2, which are widely expressed and present in white adipose tissue. DGAT-1 is most highly expressed in the small intestine, whereas DGAT-2 is primarily expressed in the liver. Therefore, the selective inhibition of DGAT-1 has become an attractive target with growing potential for the treatment of obesity and type II diabetes. Furthermore, DGAT-2 has been suggested as a new target for the treatment of DGAT-2-related liver diseases including hepatic steatosis, hepatic injury, and fibrosis. In view the discovery of drugs that target DGAT, herein we attempt to provide insight into the scope and further reasons for optimization of DGAT inhibitors. Pathway barricades: Herein we summarize all potent diacylglycerol acyltransferase (DGAT) inhibitors derived from various natural sources (i.e., plants and microorganisms) and from synthetic chemical libraries. This review emphasizes the functions of DGATs along with their importance as therapeutic targets for the treatment of metabolic disorders.

Original languageEnglish
Pages (from-to)2410-2424
Number of pages15
Issue number11
Publication statusPublished - 2014 Aug 17

Bibliographical note

Publisher Copyright:
© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


  • DGAT
  • diacylglycerol acyltransferase
  • metabolic disorders
  • small-molecule inhibitors
  • triacylglycerides

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry


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