Regulation of signal transduction by calcitonin gene-related peptide receptors

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Abstract

Calcitonin gene-related peptide (CGRP) plays a pivotal role in migraine, activating its cognate receptor to initiate intracellular signalling. This atypical receptor comprises a distinct assembly, made up of a G protein-coupled receptor (GPCR), a single transmembrane protein, and an additional protein that is required for Ga(s) coupling. By altering the expression of individual receptor components, it might be possible to adjust cellular sensitivity to CGRP. In recognition of the increasing clinical significance of CGRP receptors, it is timely to review the signalling pathways that might be controlled by this receptor, how the activity of the receptor itself is regulated, and our current understanding of the molecular mechanisms involved in these processes. Like many GPCRs, the CGRP receptor appears to be promiscuous, potentially coupling to several G proteins and intracellular pathways. Their precise composition is likely to be cell type-dependent, and much work is needed to ascertain their physiological significance.

Details

Original languageEnglish
Pages (from-to)476-483
Number of pages8
JournalTrends in Pharmacological Sciences
Volume31
Issue number10
Early online date13 Jul 2010
DOIs
Publication statusPublished - Oct 2010

    Keywords

  • animals, calcitonin gene-related peptide, drug delivery systems, gene expression regulation, humans, migraine disorders, calcitonin gene-related peptide receptors, signal transduction

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