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

17 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

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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.
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