Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

Holly Rosena Yeatman, Jonathan Robert David Lane, Kwok Ho Christopher Choy, Nevin Lambert, Patrick Sexton, Arthur Christopoulos, Meritxell Canals

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)15856 - 15866
Number of pages11
JournalThe Journal of Biological Chemistry
Volume289
Issue number22
DOIs
Publication statusPublished - 2014

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