Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective

被引:212
作者
Milligan, G [1 ]
机构
[1] Univ Glasgow, Inst Biomed & Life Sci, Div Biochem & Mol Biol, Mol Pharmacol Grp, Glasgow G12 8QQ, Lanark, Scotland
关键词
D O I
10.1124/mol.64.6.1271
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Over the last decade, the ability to detect agonist-independent signal transduction by G protein-coupled receptors has in turn resulted in the detection and study of ligands able to block this activity. Such ligands are generically described as inverse agonists. Considerable attention has recently been devoted to the presence and roles of endogenous antagonist/inverse agonists and the concept that inverse agonists may have specific therapeutic benefits compared with neutral antagonists.
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页码:1271 / 1276
页数:6
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