Allosteric activation of plasma membrane receptors - physiological implications and structural origins

被引：11

作者：

Conigrave, AD ^{[1
]}

Franks, AH ^{[1
]}

机构：

[1] Univ Sydney, Sch Mol & Microbial Biosci, Sydney, NSW 2006, Australia

来源：

PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY | 2003年 / 81卷 / 03期

基金：

英国医学研究理事会;

关键词：

plasma membrane; receptor; metabotropic receptor; G-protein-coupled receptor; allosteric modulator; agonist; conformational induction; conformational selection;

D O I：

10.1016/S0079-6107(03)00020-8

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Allosteric modulation of receptors has physiological not just pharmacological significance. Thus, the chemical context in which an agonist signal is received can have a major impact on the nature of the physiological response by modifying receptor sensitivity and/or maximal activity-even the nature of the signalling response. In addition, recognising that an endogenous activator is the allosteric modulator of a known receptor, rather than the agonist of a novel receptor, has the potential to solve, in dramatic fashion, key physiological questions. What is an allosteric modulator and why are allosteric effects on receptors so diverse and frequently complex? What is the scope of allosteric effects? Can the existence of endogenous modulators be predicted from a receptor's amino acid sequence? How should screening for endogenous allosteric modulators be undertaken? These questions form the framework of this mini-review on physiological and structural aspects of receptor allostery. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：219 / 240

页数：22

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