Article
Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action.
Assay and drug development technologies - 1 Apr 2003
Cotecchia Susanna, Fanelli Francesca, Costa Tommaso
Abstract excerpt
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...
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