Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

Yeatman, Holly R.; Lane, J. Robert; Choy, Kwok Ho Christopher; Lambert, Nevin A.; Sexton, Patrick M.; Christopoulos, Arthur; Canals, Meritxell

Abstract

Background: The effects of allosteric modulators on G protein-coupled receptor trafficking are largely unknown. Results: The allosteric ligand BQCA modulates M1 mAChR arrestin recruitment and receptor trafficking. Conclusion: M1 mAChR trafficking is arrestin- and G protein-dependent and modulated by BQCA. Significance: The impact of allosteric modulators on receptor trafficking needs to be assessed when considering this family of ligands as potential chronic therapies. © 2014 by The American Society for Biochemistry and Molecular Biology, Inc. Published in the U.S.A.

Citation

Yeatman, H. R., Lane, J. R., Choy, K. H. C., Lambert, N. A., Sexton, P. M., Christopoulos, A., & Canals, M. (2014). Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking. Journal of Biological Chemistry, 289(22), 15856-15866. https://doi.org/10.1074/jbc.M113.536672

• Journal Article Type: Article
• Acceptance Date: Apr 14, 2014
• Online Publication Date: May 30, 2014
• Publication Date: May 30, 2014
• Deposit Date: Jan 17, 2020
• Journal: Journal of Biological Chemistry
• Print ISSN: 0021-9258
• Electronic ISSN: 1083-351X
• Publisher: American Society for Biochemistry and Molecular Biology
• Peer Reviewed: Peer Reviewed
• Volume: 289
• Issue: 22
• Pages: 15856-15866
• DOI: https://doi.org/10.1074/jbc.M113.536672
• Keywords: Biochemistry; Biology; Allosteric modulation; Allosteric modulators; Arrestins; G protein coupled receptors; Muscarinic acetylcholine receptors; Receptor trafficking; Subcellular trafficking; Ligands; benzyl quinolone carboxylic acid; beta arrestin 1; bet
• Public URL: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84901708225&doi=10.1074%2fjbc.M113.536672&partnerID=40&md5=7f6a1afd0afb36332ed8ae68dfee2d8e