Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

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

Research output: Contribution to journalArticle

16 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.

Original languageEnglish (US)
Pages (from-to)15856-15866
Number of pages11
JournalJournal of Biological Chemistry
Volume289
Issue number22
DOIs
StatePublished - May 30 2014

Fingerprint

Arrestin
Muscarinic Receptors
Modulators
Modulation
Ligands
G-Protein-Coupled Receptors
GTP-Binding Proteins
Therapeutics

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

Cite this

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.

In: Journal of Biological Chemistry, Vol. 289, No. 22, 30.05.2014, p. 15856-15866.

Research output: Contribution to journalArticle

Yeatman, Holly R. ; Lane, J. Robert ; Choy, Kwok Ho Christopher ; Lambert, Nevin A ; Sexton, Patrick M. ; 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{76e94ac5d4d549898b5e5ce56963e0c1,
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.",
author = "Yeatman, {Holly R.} and Lane, {J. Robert} and Choy, {Kwok Ho Christopher} and Lambert, {Nevin A} and Sexton, {Patrick M.} and Arthur Christopoulos and Meritxell Canals",
year = "2014",
month = "5",
day = "30",
doi = "10.1074/jbc.M113.536672",
language = "English (US)",
volume = "289",
pages = "15856--15866",
journal = "Journal of Biological Chemistry",
issn = "0021-9258",
publisher = "American Society for Biochemistry and Molecular Biology Inc.",
number = "22",

}

TY - JOUR

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

AU - Yeatman, Holly R.

AU - Lane, J. Robert

AU - Choy, Kwok Ho Christopher

AU - Lambert, Nevin A

AU - Sexton, Patrick M.

AU - Christopoulos, Arthur

AU - Canals, Meritxell

PY - 2014/5/30

Y1 - 2014/5/30

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.

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.

UR - http://www.scopus.com/inward/record.url?scp=84901708225&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84901708225&partnerID=8YFLogxK

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 - 0021-9258

IS - 22

ER -