Regulating expression and function of G-protein-linked receptors

被引:34
作者
Karoor, V [1 ]
Shih, ML [1 ]
Tholanikunnel, B [1 ]
Malbon, CC [1 ]
机构
[1] SUNY STONY BROOK, MED CTR, DEPT MOLEC PHARMACOL, DIABET & METAB DIS RES PROGRAM, STONY BROOK, NY 11794 USA
关键词
D O I
10.1016/0301-0082(96)00004-4
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
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. Copyright (C) 1996 Elsevier Science Ltd
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页码:555 / 568
页数:14
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