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

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.