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In vitro profiling of orphan G protein coupled receptor (GPCR) constitutive activity

Br J Pharmacol. 2021-05; 
Lyndsay R Watkins, Cesare Orlandi
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摘要

background and purpose: Members of the GPCR family are targeted by a significant fraction of the available FDA-approved drugs. However, the physiological role and pharmacological properties of many GPCRs remain unknown, representing untapped potential in drug design. Of particular interest are ~100 less-studied GPCRs known as orphans because their endogenous ligands are unknown. Intriguingly, disease-causing mutations identified in patients, together with animal studies, have demonstrated that many orphan receptors play crucial physiological roles and, thus, represent attractive drug targets. experimental approach: The majority of deorphanized GPCRs demonstrate coupling to G . However, a limited number of techn... More

关键词

GPCR, cell signalling, constitutive activity, molecular pharmacology