α_1-肾上腺素受体结构改变影响其生物学活性及生理功能的研究进展  

Research progress on structural modification of α_1-adrenergic receptor influencing its biological activities and its physiological function

作　　者：马力 杨泽平 母茜 邵钰婷 杨洋[1] 安输[1] 郭晓汐 郝倩[1] 徐天瑞[1] 刘莹[1] MA Li;YANG Ze-ping;MU Xi;SHAO Yu-ting;YANG Yang;AN Shu;GUO Xiao-xi;HAO Qian;XU Tian-rui;LIU Ying(Cell Signaling Lab, Faculty of Life Science and Technology, Kunming Universityof Science and Technology, Kunming 650500, China)

机构地区：[1]昆明理工大学生命科学与技术学院细胞信号传导实验室,云南昆明650500

出　　处：《中国药理学通报》2019年第6期748-752,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81560455;81460417;81460253)

摘　　要：α_1-肾上腺素受体(α_1-ARs)属于G蛋白偶联受体,包含α_1A、α_1B、α_(1D)3种亚型。α_1-ARs结构改变可导致其生理功能的改变。该文总结了α_1-ARs羧基端截短、二聚化、别构效应和点突变的结构改变,导致其内吞、磷酸化、脱敏以及对激动剂的亲和力等生理功能的变化。The α 1-adrenergic receptor(α 1-AR) belongs to G-protein coupled receptors (GPCRs) and contains three subtypes, namely α 1A ,α 1B and α 1D . Studies have shown that structural changes in the α 1-ARs receptor can lead to changes in their physiological functions. In the present study, we summarize the structural changes in four aspects of α 1-ARs receptors, including carboxy-terminal truncation, dimerization, allosteric effects, and point mutations that lead to endocytosis, phosphorylation, desensitization, and affinity for agonists.

关 键 词：Α1-肾上腺素受体 羧基末端 二聚化 别构效应 点突变 生理功能 

分 类 号：R392.11[医药卫生—免疫学]