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

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
JournalJournal of Biological Chemistry
Volume289
Issue number22
DOIs
Publication statusPublished - 2014

Cite this

Yeatman, Holly Rosena ; Lane, Jonathan Robert David ; Choy, Kwok Ho Christopher ; Lambert, Nevin ; Sexton, Patrick ; Christopoulos, Arthur ; Canals, Meritxell. / Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking. In: Journal of Biological Chemistry. 2014 ; Vol. 289, No. 22. pp. 15856 - 15866.
@article{c76a4b24968a464aa1e169cdae791fce,
title = "Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking",
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.",
author = "Yeatman, {Holly Rosena} and Lane, {Jonathan Robert David} and Choy, {Kwok Ho Christopher} and Nevin Lambert and Patrick Sexton and Arthur Christopoulos and Meritxell Canals",
year = "2014",
doi = "10.1074/jbc.M113.536672",
language = "English",
volume = "289",
pages = "15856 -- 15866",
journal = "Journal of Biological Chemistry",
issn = "1083-351X",
publisher = "American Society for Biochemistry and Molecular Biology",
number = "22",

}

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking. / Yeatman, Holly Rosena; Lane, Jonathan Robert David; Choy, Kwok Ho Christopher; Lambert, Nevin; Sexton, Patrick; Christopoulos, Arthur; Canals, Meritxell.

In: Journal of Biological Chemistry, Vol. 289, No. 22, 2014, p. 15856 - 15866.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

AU - Yeatman, Holly Rosena

AU - Lane, Jonathan Robert David

AU - Choy, Kwok Ho Christopher

AU - Lambert, Nevin

AU - Sexton, Patrick

AU - Christopoulos, Arthur

AU - Canals, Meritxell

PY - 2014

Y1 - 2014

N2 - 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.

AB - 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.

UR - http://www.jbc.org/content/289/22/15856.full.pdf+html

U2 - 10.1074/jbc.M113.536672

DO - 10.1074/jbc.M113.536672

M3 - Article

VL - 289

SP - 15856

EP - 15866

JO - Journal of Biological Chemistry

JF - Journal of Biological Chemistry

SN - 1083-351X

IS - 22

ER -