Karoor V, Shih M, Tholanikunnel B, Malbon C C
Department of Molecular Pharmacology, University Medical Center, SUNY/Stony Brook 11794-8651, USA.
Prog Neurobiol. 1996 Apr;48(6):555-68. doi: 10.1016/0301-0082(96)00004-4.
G-protein-linked receptors constitute a populous family of heptahelical, membrane-localized receptors for hormones, drugs and neurotransmitters that activate a diverse and smaller subset of effectors, including adenylylcyclases, phospholipases and various ion channels. The expression and functional status of G-protein-linked receptors is highly regulated. Expression is controlled largely by activation or repression of the genes encoding the receptors, balanced by post-transcriptional mechanisms such as destabilization of receptor mRNA. Agonist-induced down-regulation of receptors involves both transcriptional and post-transcriptional controls. Gene structure reveals details of promoters as well as determinants for mRNA stability. Post-translational regulation of G-protein-linked receptors is dominated by protein phosphorylation. G-protein-linked receptors are substrates not only for protein kinase A, protein kinase C and receptor-specific kinases, but also for growth factor receptors with intrinsic tyrosine kinase activity. Recent advances in the study of beta-adrenergic receptors (beta ARs) illuminate new dynamic features of receptor regulation, central to our understanding of neurobiology.
G蛋白偶联受体构成了一个庞大的七螺旋膜定位受体家族，这些受体可识别激素、药物和神经递质，激活包括腺苷酸环化酶、磷脂酶和各种离子通道在内的多种效应器的一个多样化且较小的子集。G蛋白偶联受体的表达和功能状态受到高度调控。表达主要由编码受体的基因的激活或抑制控制，并通过转录后机制（如受体mRNA的不稳定）保持平衡。激动剂诱导的受体下调涉及转录和转录后控制。基因结构揭示了启动子的细节以及mRNA稳定性的决定因素。G蛋白偶联受体的翻译后调控主要由蛋白质磷酸化主导。G蛋白偶联受体不仅是蛋白激酶A、蛋白激酶C和受体特异性激酶的底物，也是具有内在酪氨酸激酶活性的生长因子受体的底物。β肾上腺素能受体（βARs）研究的最新进展揭示了受体调控的新动态特征，这对于我们理解神经生物学至关重要。
