Uncoupling of G-Protein Coupled Receptors in vivo: Insights from Transgenic Mice

摘要: Heart failure is a problem of increasing importance in medicine. An important characteristic heart reduced agonist-stimulated adenylyl cyclase activity (receptor desensitization) due to both diminished receptor number down regulation) and impaired function uncoupling). These changes the s-adrenergic (s-AR) system, may part account for some abnormalities contractile this disease. Myocardial contraction closely regulated by Gprotein coupled receptors through action second messenger cAMP. The s-AR themselves are set specific kinases, termed Gprotein-coupled kinases (GRKs). study complex system vivo has recently been advanced development transgenic gene targeted (“knockout”) mouse models. Combining technology with sophisticated physiological measurements cardiac hemodynamics an extremely powerful strategy regulation myocardial contractility normal failing heart.