DGAT inhibitors for obesity.
Obesity is characterized by the accumulation of triacylglycerol in adipocytes. Diacylglycerol acyltransferase (DGAT) catalyzes the final reaction of triacylgycerol synthesis. Two isozymes of DGAT, DGAT1 and DGAT2, have been reported. Increased DGAT2 activity has a role in steatosis, while DGAT1 plays a role in very (V)LDL synthesis; increased plasma VLDL concentrations may promote obesity and thus DGAT1 is considered a potential therapeutic target of inhibition for obesity control. Several DGAT inhibitors of natural and synthetic origin have been reported, and their future prospect as anti-obesity drugs is discussed in this review.
Matsuda
Daisuke
D
Kitasato University, School of Pharmacy, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
Tomoda
Hiroshi
H
D017667:Adipocytes / Q000378:metabolism; D000818:Animals; D019440:Anti-Obesity Agents / Q000627:therapeutic use*; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000502:physiology; D005234:Fatty Liver / Q000378:metabolism; D006801:Humans; D008079:Lipoproteins, VLDL / Q000097:blood; D009765:Obesity / Q000188:drug therapy* / Q000378:metabolism
D019440:Anti-Obesity Agents; D008079:Lipoproteins, VLDL; C494881:DGAT1 protein, human; C494885:DGAT2 protein, human; D051048:Diacylglycerol O-Acyltransferase