Constitutively active G protein-coupled receptor mutants: Implications on receptor function and drug action

被引:12
作者
Cotecchia, S
Fanelli, F
Costa, T
机构
[1] Univ Lausanne, Inst Pharmacol & Toxicol, CH-1005 Lausanne, Switzerland
[2] Univ Modena & Reggio Emilia, Dulbecco Telethon Inst, Modena, Italy
[3] Univ Modena & Reggio Emilia, Dept Chem, Modena, Italy
[4] Ist Super Sanita, I-00161 Rome, Italy
关键词
D O I
10.1089/15406580360545125
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Mutations of GPCRs can increase their constitutive (agonist-independent) activity. Some of these mutations have been artificially introduced by site-directed mutagenesis; others occur spontaneously in human diseases. The analysis of constitutively active GPCR mutants has attracted a large interest in the past decade, providing an important contribution to our understanding of the molecular mechanisms underlying receptor function and drug action.
引用
收藏
页码:311 / 316
页数:6
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