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Novel pharmacological applications of G-protein-coupled receptor-G protein fusions

Milligan, Graeme; Parenty, Geraldine; Stoddart, Leigh A; Lane, J Robert

Authors

Graeme Milligan

Geraldine Parenty

Leigh A Stoddart

ROB LANE ROB.LANE@NOTTINGHAM.AC.UK
Associate Professor



Abstract

Single, bi-functional polypeptides consisting of a G-protein-coupled receptor (GPCR) linked directly to a G protein alpha subunit have been employed for a number of years to study many aspects of signal initiation, including the roles of post-translational modifications, effects of mutations in both receptor and G protein and in the de-orphanisation of novel G-protein-coupled receptors. Recently, they have been used to improve signal-to-background in ligand assay screens and to study both agonist-directed signal trafficking and distinct conformational states of receptors. As well as such novel concepts in pharmacology, G-protein-coupled receptor-G protein fusions have recently been employed to examine receptor homo-dimerisation and hetero-dimerisation and are beginning to be used to explore allosteric effects within GPCR hetero-dimers.

Journal Article Type Article
Online Publication Date Aug 6, 2007
Publication Date 2007-10
Deposit Date Apr 22, 2020
Print ISSN 1471-4892
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 7
Issue 5
Pages 521-526
DOI https://doi.org/10.1016/j.coph.2007.06.007
Public URL http://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=17689289&retmode=ref&cmd=prlinks
Publisher URL https://www.sciencedirect.com/science/article/abs/pii/S1471489207001075