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Agonist induction and conformational selection during activation of a G-protein-coupled receptor

✍ Scribed by László Hunyady; Georges Vauquelin; Patrick Vanderheyden

Book ID
117341007
Publisher
Elsevier Science
Year
2003
Tongue
English
Weight
403 KB
Volume
24
Category
Article
ISSN
0165-6147

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✦ Synopsis

Substitutions of Asn111 of the AT 1 angiotensin receptor and mutations of the corresponding amino acids in other G-protein-coupled receptors (GPCRs) cause constitutive receptor activation. Ligand binding and signalling of constitutively active mutant GPCRs are discussed and similarities and differences during the activation of amine and peptide GPCRs are identified. Studies using the AT 1 receptor suggest that conformational selection is not sufficient to explain the mechanism of receptor activation, and that agonist binding to the receptor provides energy to induce activation of the receptor. Because agonist binding also actively facilitates the conformational rearrangements leading to activation of other GPCRs we propose that agonist induction should be considered as a general mechanism of GPCR activation.

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✍ Hui Zheng; Horace H. Loh; Ping-Yee Law 📂 Article 📅 2010 🏛 John Wiley and Sons 🌐 English ⚖ 118 KB 👁 1 views

## Abstract Agonist‐selective signaling or ligand‐biased signaling of G protein‐coupled receptor (GPCR) has become the focus of an increasing number of laboratories. The principle of this concept is that agonist possesses different abilities to activate different signaling pathways. Current review