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.
Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action / S., Cotecchia; Fanelli, Francesca; T., Costa. - In: ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES. - ISSN 1540-658X. - ELETTRONICO. - 1:2(2003), pp. 311-316. [10.1089/15406580360545125]
Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action
FANELLI, Francesca;
2003
Abstract
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.
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