G蛋白偶联受体激酶在心血管疾病中的作用

Role of G protein-coupled receptor kinases in cardiovascular diseases

G-protein-coupled receptors (GPCRs) are hitherto the largest family of membrane receptors. They activate associated heterotrimeric G-proteins and participate in the regulation of intracellular signaling pathways, which are accomplished via ligand binding to them. G-protein-coupled receptor kinases (GRKs) are key modulators of GPCR signaling. GRKs, in concert with β-arrestins, classically lead to desensitization and internalization of GPCR, thus preventing hyperactivation of GPCR second messenger cascades. Changes in the GRKs expression and regulation have featured prominently in many cardiovascular diseases, including heart failure, myocardial infarction, cardiac hypertrophy, and hypertension. Intensively studying the role of GRKs in cardiovascular diseases contributes to expounding the mechanism of correlated diseases. Herein, we review the role of GRKs in cardiovascular pathophysiology.