Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development.

Show simple item record Archbold, JK en Flanagan, Jack en Watkins, HA en Gingell, Joseph en Hay, Deborah en
dc.coverage.spatial England en 2012-03-14T20:55:01Z en 2011-10 en
dc.identifier.citation Trends in Pharmacological Sciences 32(10):591-600 Oct 2011 en
dc.identifier.uri en
dc.description.abstract Secretin family G protein-coupled receptors (GPCRs) are important therapeutic targets for migraine, diabetes, bone disorders, inflammatory disorders and cardiovascular disease. They possess a large N-terminal extracellular domain (ECD) known to be the primary ligand-binding determinant. Structural determination of several secretin family GPCR ECDs in complex with peptide ligands has been achieved recently, providing insight into the molecular determinants of hormone binding. Some secretin family GPCRs associate with receptor activity-modifying proteins (RAMPs), resulting in changes to receptor pharmacology. Recently, the first crystal structure of a RAMP ECD in complex with a secretin family GPCR was solved, revealing the elegant mechanism governing receptor selectivity of small molecule antagonists of the calcitonin gene-related peptide (CGRP) receptor. Here we review the structural basis of ligand binding to secretin family GPCRs, concentrating on recent progress made on the structural basis of RAMP-modified GPCR pharmacology and its implications for rational drug design. en
dc.language eng en
dc.publisher Elsevier en
dc.relation.ispartofseries Trends in Pharmacological Sciences en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. Details obtained from: en
dc.rights.uri en
dc.subject Drug Design en
dc.subject Humans en
dc.subject Receptor Activity-Modifying Proteins en
dc.subject Receptors, G-Protein-Coupled en
dc.subject Secretin en
dc.title Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development. en
dc.type Journal Article en
dc.identifier.doi 10.1016/ en
pubs.issue 10 en
pubs.begin-page 591 en
pubs.volume 32 en
dc.rights.holder Copyright: Elsevier en
dc.identifier.pmid 21722971 en
pubs.end-page 600 en
dc.rights.accessrights en
pubs.subtype Review en
pubs.elements-id 232840 en Medical and Health Sciences en Medical Sciences en Pharmacology en Science en Biological Sciences en Science Research en Maurice Wilkins Centre (2010-2014) en
dc.identifier.eissn 1873-3735 en
dc.identifier.pii S0165-6147(11)00096-4 en
pubs.record-created-at-source-date 2012-03-15 en
pubs.dimensions-id 21722971 en

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