Journal
CHEMMEDCHEM
Volume 9, Issue 11, Pages 2410-2424Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201402069
Keywords
DGAT; diacylglycerol acyltransferase; metabolic disorders; small-molecule inhibitors; triacylglycerides
Categories
Funding
- National Research Foundation (NRF) - Korean Government [2012M3A9C1053532, 2012M3A9B4028787]
- GRRC program of Gyeonggi Province [GRRC-DONG-GUK2013-B02]
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Metabolic diseases such as atherogenic dyslipidemia, hepatic steatosis, obesity, and typeII 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 typeII 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.
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