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Critical Reviews™ in Neurobiology
SJR: 0.121

ISSN Print: 0892-0915
ISSN Online: 2375-0014

Archives: Volume 10, 1996 to Volume 20, 2008

Critical Reviews™ in Neurobiology

DOI: 10.1615/CritRevNeurobiol.v10.i1.40
pages 69-99

Molecular Biology of Muscarinic Acetylcholine Receptors

Jurgen Wess
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bldg. 8A, Rm. B1A-09, Bethesda, Maryland 20892


Following the molecular cloning of five distinct muscarinic acetylcholine receptor (mAChR) genes, the last decade has witnessed an explosion of new knowledge about how mAChRs function at a molecular level. These studies have been greatly facilitated by the molecular characterization of the many components of the signal transduction pathways activated upon mAChR stimulation. Molecular genetic and biochemical approaches have considerably advanced our knowledge about how mAChRs are assembled, how they bind ligands, and which structural elements on the mAChRs are critical for G protein coupling. In addition, the molecular mechanisms involved in the regulation of mAChR activity (including mAChR sequestration, down-regulation, and phosphorylation) have been explored in great detail. Since the mAChRs are typical members of the superfamily of G protein-coupled receptors, the information gathered with this class of receptors should be of broad general relevance.

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