血管疾病成为威胁人类健康头号杀手,心血管受体在心血管疾病的发生、发展及预防和治疗中具有举足轻重的地位。β-肾上腺素受体作为 G 蛋白偶联受体家族的成员,是心血管药物最重要的靶点之一。β-肾上腺素受体阻滞剂被认为是继洋地黄后药物防治心脏疾病的最伟大突破,其在心血管领域的研究和应用一直是被关注的热点。2012年度诺贝尔化学奖再次授予了β-肾上腺素受体的研究。随着研究的深入,人们发现β-肾上腺素受体接受着细胞内调控蛋白的精密调控,不同调控蛋白介导着受体不同的生理信号通路和病理性信号通路。基于这些发现,近年来提出了受体功能选择性的配体药物,这也将成为未来药物的研究方向。本文综述了β-肾上腺素受体调节蛋白及相关信号通路及功能。
Vascular diseases has become a top killer of human health,and cardiovascular receptors are pivotal in the occurrence,development,prevention and treatment of cardiovascular diseases.As for the important member of G protein-coupled receptor,β-adrenergic receptor is undoubtedly a most important target of cardiovascular drugs.Being the hot spot in the cardiovascular research and application,β-ad-renergic receptor blocker has been considered as the greatest breakthrough for the prevention and cure of cardiovascular disease after digitalis.The 201 2 Nobel Prize in chemistry was awarded again to the re-searchers on β-adrenergic receptors.Extensive researchs show that β-adrenergic receptors are precisely regulated by different regulatory proteins in cells in the transduction of different physiological and patho-logical signaling pathways.Based on these findings,function-selective ligands recently arise in the recep-tor research and will be the new chance of drug discovery.In this article we reviewed the related signal pathways and functions of β-adrenergic receptor regulatory proteins.