Lipogenic enzymes as therapeutic targets for obesity and diabetes.

Publisher: Bentham Science Publishers Country of Publication: United Arab Emirates NLM ID: 9602487 Publication Model: Print Cited Medium: Internet ISSN: 1873-4286 (Electronic) Linking ISSN: 13816128 NLM ISO Abbreviation: Curr Pharm Des Subsets: MEDLINE

Publication: Saif Zone, Sharjah, U.A.E. : Bentham Science Publishers
Original Publication: Schiphol, The Netherlands : Bentham Science Publishers, c1995-

Lipogenesis*; Acetyl-CoA Carboxylase/*metabolism ; Adipocytes/*enzymology ; Adipose Tissue/*enzymology ; Diabetes Mellitus/*enzymology ; Diabetes Mellitus, Type 2/*enzymology ; Enzyme Inhibitors/*pharmacology ; Obesity/*enzymology; Acetyl-CoA Carboxylase/antagonists & inhibitors ; Adipocytes/metabolism ; Adipogenesis ; Adipose Tissue/metabolism ; Animals ; Diabetes Mellitus/drug therapy ; Diabetes Mellitus/metabolism ; Diabetes Mellitus, Type 2/drug therapy ; Diabetes Mellitus, Type 2/metabolism ; Diacylglycerol O-Acyltransferase/antagonists & inhibitors ; Diacylglycerol O-Acyltransferase/metabolism ; Disease Models, Animal ; Enzyme Inhibitors/therapeutic use ; Fatty Acid Synthases/antagonists & inhibitors ; Fatty Acid Synthases/metabolism ; Humans ; Molecular Targeted Therapy ; Obesity/drug therapy ; Obesity/metabolism ; Stearoyl-CoA Desaturase/antagonists & inhibitors ; Stearoyl-CoA Desaturase/metabolism

Since storage of excess fat in peripheral tissues is a contributing factor leading to obesity and type II diabetes, many investigators are studying the key lipid metabolizing enzymes found in adipose tissue as drug targets to reduce excess fat. The availability of cultured cell lines and primary stem cells, preadipocyetes, and adipocytes has facilitated therapeutic approaches aimed at targeting fat storage. This includes developing inhibitors for enzymes regulating lipogenesis in these cells, such as acetyl-CoA carboxylase, fatty acid synthase, diacylgycerol acyl transferase, and stearoyl CoA desaturase. High level expression of each protein is often used to confirm stem cells have undergone adipogenesis. Inhibition of these enzymes often leads to reduced fat cell fat differentiation and lipid synthesis and may also contribute to increased fat oxidation and energy expenditure. This article reviews developments in pharmaceutical research on these enzymes, with particular emphasis on the role of the enzymes in adipose tissue metabolism.

0 (Enzyme Inhibitors)
EC 1.14.19.1 (Stearoyl-CoA Desaturase)
EC 2.3.1.20 (Diacylglycerol O-Acyltransferase)
EC 2.3.1.85 (Fatty Acid Synthases)
EC 6.4.1.2 (Acetyl-CoA Carboxylase)

Date Created: 20110308 Date Completed: 20110727 Latest Revision: 20190728

20221213

10.2174/138161211795164185

21375498