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Nat Rev Drug Discov. 2014 Jul;13(7):549-60. doi: 10.1038/nrd4295. Epub 2014 Jun 6.

Muscarinic acetylcholine receptors: novel opportunities for drug development.

Author information

1
1] Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, California 94305, USA. [2] Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, USA.
2
Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, California 94305, USA.
3
Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, US National Institutes of Health, Bethesda, Maryland 20892-0810, USA.
4
Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria 3052, Australia.

Abstract

The muscarinic acetylcholine receptors are a subfamily of G protein-coupled receptors that regulate numerous fundamental functions of the central and peripheral nervous system. The past few years have witnessed unprecedented new insights into muscarinic receptor physiology, pharmacology and structure. These advances include the first structural views of muscarinic receptors in both inactive and active conformations, as well as a better understanding of the molecular underpinnings of muscarinic receptor regulation by allosteric modulators. These recent findings should facilitate the development of new muscarinic receptor subtype-selective ligands that could prove to be useful for the treatment of many severe pathophysiological conditions.

PMID:
24903776
PMCID:
PMC5818261
DOI:
10.1038/nrd4295
[Indexed for MEDLINE]
Free PMC Article

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