Muscarinic receptor oligomerization

NEUROPHARMACOLOGY

卷:136

Review

Marsango, Sara¹  Ward, Richard J.¹  Alvarez-Curto, Elisa¹  Milligan, Graeme¹ 

[1] Univ Glasgow, Coll Med Vet & Life Sci, Inst Mol Cell & Syst Biol, Ctr Translat Pharmacol, Glasgow G12 8QQ, Lanark, Scotland

关键词: Muscarinic acetylcholine receptor;    Quaternary structure;    Dimerization;    Oligomerization;    Ligand regulation;   

DOI  :  10.1016/j.neuropharm.2017.11.023

来源: Elsevier

【 摘 要 】

G protein-coupled receptors (GPCRs) have been classically described as monomeric entities that function by binding in a 1:1 stoichiometric ratio to both ligand and downstream signalling proteins. However, in recent years, a growing number of studies has supported the hypothesis that these receptors can interact to form dimers and higher order oligomers although the molecular basis for these interactions, the overall quaternary arrangements and the functional importance of GPCR oligomerization remain topics of intense speculation. Muscarinic acetylcholine receptors belong to class A of the GPCR family. Each muscarinic receptor subtype has its own particular distribution throughout the central and peripheral nervous systems. In the central nervous system, muscarinic receptors regulate several sensory, cognitive, and motor functions while, in the peripheral nervous system, they are involved in the regulation of heart rate, stimulation of glandular secretion and smooth muscle contraction. Muscarinic acetylcholine receptors have long been used as a model for the study of GPCR structure and function and to address aspects of GPCR dimerization using a broad range of approaches. In this review, the prevailing knowledge regarding the quaternary arrangement for the various muscarinic acetylcholine receptors has been summarized by discussing work ranging from initial results obtained using more traditional biochemical approaches to those generated with more modern biophysical techniques. This article is part of the Special Issue entitled 'Neuropharmacology on Muscarinic Receptors'. (C) 2017 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).

【 授权许可】

Free