Role of the sulfonylurea receptor in regulating human adipocyte metabolism

摘要: A regulatory role for intracellular Ca2+ ([Ca2+]i) in adipocyte lipogenesis, lipolysis and triglyceride accumulation has been demonstrated. Compounds acting on the pancreatic sulfonylurea receptor (SUR) to increase (e.g., glibenclamide) or decrease diazoxide) [Ca2+]i cause corresponding increases decreases weight gain. However, these gain loss effects have attributed insulin release rather than primary of compounds SUR its associated K(ATP) channel. Accordingly, we evaluated direct human regulating metabolism. We used RT-PCR with primers a highly conserved region SUR1 demonstrate that adipocytes express SUR1. The PCR product was confirmed by sequence analysis as probe expression Northern blot analysis. Adipocytes exhibited glibenclamide dose-responsive (0-20 microM) (P<0.05). Similarly, (10 caused 67% fatty acid synthase activity (P<0.001), 48% glycerol-3-phosphate dehydrogenase (P<0.01) 68% inhibition (P<0.01), whereas diazoxide completely prevented each effects. These data regulates and, consequently, exerts coordinate control over lipogenesis lipolysis. may represent an important target development therapeutic interventions obesity.