心脏β肾上腺素受体信号转导研究与相关药物研发  

β-Adrenergic Receptors in the Heart:Signal Transduction and Drug Discovery

作　　者：王怡玫[1] 胡耀豪 肖瑞平[1,3] 

机构地区：[1]北京大学分子医学研究所,北京100871 [2]沈阳药科大学生命科学与生物制药学院,辽宁沈阳110016 [3]北京大学-清华大学生命科学联合中心,北京100871

出　　处：《药学进展》2017年第3期170-176,共7页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金(No.81673355)

摘　　要：β肾上腺素受体作为重要的G蛋白偶联受体家族成员,在血液循环、代谢调节、肌肉收缩和舒张中都具有重要的作用。在心脏中,急性激活β肾上腺素受体能够促进心脏功能,持续性激活β肾上腺素受体在心脏重构的病理生理过程中具有重要作用。心脏中的β肾上腺素受体包括3个亚型:β_1肾上腺素受体、β_2肾上腺素受体和β_3肾上腺素受体。文章重点讨论了β_1和β_2肾上腺素受体二者在心脏中不同甚至截然相反的作用。在此基础上,提出基于β肾上腺素受体信号转导亚型特异性的心衰治疗新方法。As important members of the G protein-coupled receptor superfamily, β-adrenergic receptors are involved in the regulation of key physiological processes such as circulation, metabolism and muscle contraction/relaxation. β-Adrenergic receptors are abundantly expressed in the heart and include three subtypes： β1, β2 and β3. Acute stimulation of these receptors enhances cardiac function while chronic stimulation leads to both structural and functional abnormalities of the heart. In this review, we discussed the differences between the signaling pathways of β1-adrenergic receptor and β2-adrenergic receptor in the heart and proposed a novel strategy for treating heart failure based on subtype-speci c β-adrenergic receptor signal transduction.

关 键 词：心力衰竭 Β1肾上腺素受体 Β2肾上腺素受体 G蛋白偶联受体激酶 信号转导 新药研发 

分 类 号：R972[医药卫生—药品]