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

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

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.

Citation

Milligan, G., Parenty, G., Stoddart, L. A., & Lane, J. R. (2007). Novel pharmacological applications of G-protein-coupled receptor-G protein fusions. Current Opinion in Pharmacology, 7(5), 521-526. https://doi.org/10.1016/j.coph.2007.06.007

• 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