Wang H Y, Hadcock J R, Malbon C C
Department of Pharmacology, SUNY, Stony Brook 11794-8651.
Receptor. 1990;1(1-2):13-32.
G-protein-linked transmembrane signaling is a major mechanism for processing information across biological membranes. Receptors that propagate signals from ligand binding to effector units via G-proteins are a populous class, including receptors for hormones, neurotransmitters, and autacoids. Much information has emerged on the structure of receptors, G-proteins, and effectors. Relatively little is known of the molecular basis underlying physiological regulation. The present article highlights the many recent advances that have permitted more detailed analysis of the regulation of one prominent member of the G-protein-linked receptor family, the beta-adrenergic receptor. Dynamic regulation of receptor function and expression is discussed with emphasis on the processes of desensitization and downregulation by agonist as well as up-regulation in response to steroids. Data are gleaned from studies of the biochemistry, cell, and molecular biology of beta-adrenergic receptors to provide a current model for discussion of receptor regulation.
G蛋白偶联跨膜信号传导是跨生物膜处理信息的主要机制。通过G蛋白将配体结合信号传递至效应器单元的受体种类繁多，包括激素、神经递质和自分泌调节因子的受体。关于受体、G蛋白和效应器的结构，已有很多信息。对于生理调节的分子基础，人们了解相对较少。本文重点介绍了许多最新进展，这些进展使人们能够对G蛋白偶联受体家族的一个重要成员——β-肾上腺素能受体的调节进行更详细的分析。文中讨论了受体功能和表达的动态调节，重点是激动剂引起的脱敏和下调过程以及类固醇引起的上调过程。数据来自对β-肾上腺素能受体生物化学、细胞和分子生物学的研究，以提供一个当前的受体调节讨论模型。
