The acetylcholine receptor: a model of an allosteric membrane protein mediating intercellular communication

Over the past 20 years the nicotinic acetylcholine receptor has become the prototype of a superfamily of ligand-gated ion channels. As a single macromolecular entity of M(r) about 300,000, the receptor protein mediates, altogether, the activation and the desensitization of the associated ion channel and the regulation of these processes by extracellular and intracellular signals. The notion is discussed that the acetylcholine receptor is a membrane-bound allosteric protein which possesses several categories of specific sites for neurotransmitters and for regulatory ligands, and undergoes conformational transitions which link these diverse sites together. At this elementary molecular level, interactions between signalling pathways may be mediated by membrane-bound allosteric receptors and/or by other categories of cytoplasmic allosteric proteins.