Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias.

doi:10.1074/jbc.M109.094011

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Article

Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias.

The Journal of biological chemistry - 5 Mar 2010

Gregory Karen J, Hall Nathan E, Tobin Andrew B, Sexton Patrick M, Christopoulos Arthur

Abstract excerpt

Muscarinic acetylcholine receptors contain at least one allosteric site that is topographically distinct from the acetylcholine, orthosteric binding site. Although studies have investigated the basis of allosteric modulation at these receptors, less is known about putative allosteric ligands that activate the receptor in their own right. We generated M(2) muscarinic acetylcholine receptor mutations in either the...

Topics

Acetylcholine
Allosteric Site
Amino Acid Sequence
Animals
Cell Line
Extracellular Signal-Regulated MAP Kinases
Guanosine 5'-O-(3-Thiotriphosphate)
Humans
Ligands
Models, Molecular

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Molecular Sequence Data

Molecular Structure

Muscarinic Agonists

Mutagenesis, Site-Directed

Mutation

Protein Isoforms

Protein Structure, Secondary

Receptor, Muscarinic M2

Source

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Identifiers

PMID: 20051519
DOI: 10.1074/jbc.M109.094011
PMCID: PMC2844194

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