• Trends Pharmacol. Sci. · Jan 2019

    Review

    New Insights into the Regulation of CGRP-Family Receptors.

    • Joseph J Gingell, Erica R Hendrikse, and Debbie L Hay.
    • School of Biological Sciences, University of Auckland, Auckland, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, University of Auckland, Auckland, New Zealand.
    • Trends Pharmacol. Sci. 2019 Jan 1; 40 (1): 71-83.

    AbstractThe calcitonin gene-related peptide (CGRP) receptor system has emerged as an important drug target for migraine. This is highlighted by the recent regulatory approval of the first drug targeting the CGRP signalling pathway, the CGRP receptor antibody erenumab. The cellular compartments in which receptors are found affects drug access and whether they can exert their effects. G protein-coupled receptors (GPCRs) were thought to signal only at the cell surface, but it is now recognised that some GPCRs, including the CGRP receptor, undergo sustained signalling from endosomes, once internalised in response to ligand. What does this mean for drugs like erenumab? This review covers recent insights into the regulation of CGRP family receptors and examines what implications this may have on drug activity.Copyright © 2018 Elsevier Ltd. All rights reserved.

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