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Review
. 2012 Nov 23;287(48):40207-15.
doi: 10.1074/jbc.R112.407668. Epub 2012 Oct 4.

The nicotinic acetylcholine receptor: the founding father of the pentameric ligand-gated ion channel superfamily

Jean-Pierre Changeux  1
Affiliations
Review

The nicotinic acetylcholine receptor: the founding father of the pentameric ligand-gated ion channel superfamily

Jean-Pierre Changeux. J Biol Chem. .

Abstract

A critical event in the history of biological chemistry was the chemical identification of the first neurotransmitter receptor, the nicotinic acetylcholine receptor. Disciplines as diverse as electrophysiology, pharmacology, and biochemistry joined together in a unified and rational manner with the common goal of successfully identifying the molecular device that converts a chemical signal into an electrical one in the nervous system. The nicotinic receptor has become the founding father of a broad family of pentameric membrane receptors, paving the way for their identification, including that of the GABA(A) receptors.

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Figures

FIGURE 1.
FIGURE 1.
Upper, binding method by equilibrium dialysis used for the identification of the nicotinic receptor. Lower, effect of the snake toxin α-BGT on binding of the nicotinic agonist [3H]decamethonium (Deca). This figure has been reprinted from Refs. (lower) and (upper).
FIGURE 2.
FIGURE 2.
Purification of the nAChR by affinity chromatography. This figure has been reprinted from Ref. .
FIGURE 3.
FIGURE 3.
First structural observation of the purified nicotinic receptor proteins from E. electricus (upper) and from purified subsynaptic membrane fragments from T. marmorata (lower). This figure has been reprinted from Ref. .
FIGURE 4.
FIGURE 4.
Minimal four-state model for the allosteric transitions of the nicotinic receptor. CB, competitive (orthosteric) blocker; NCB, noncompetitive (channel) blocker; AM, allosteric modulator; P, phosphorylation site. This figure has been reprinted from Ref. .
See this image and copyright information in PMC

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References

    1. Corringer P. J., Poitevin F., Prevost M. S., Sauguet L., Delarue M., Changeux J. P. (2012) Structure and pharmacology of pentameric receptor channels: from bacteria to brain. Structure 20, 941–956 - PubMed
    1. Nachmansohn D. (1959) The Chemical and Molecular Basis of Nerve Activity, Academic Press, New York
    1. Fenton J. W., 2nd, Singer S. J. (1965) Affinity labeling of antibodies to the p-azophenyltrimethylammonium hapten and a structural relationship among antibody active sites of different specificities. Biochem. Biophys. Res. Commun. 20, 315–320 - PubMed
    1. Changeux J. P., Podleski T. R., Wofsy L. (1967) Affinity labeling of the acetylcholine receptor. Proc. Natl. Acad. Sci. U.S.A. 58, 2063–2070 - PMC - PubMed
    1. Karlin A., Winnik M. (1968) Reduction and specific alkylation of the receptor for acetylcholine. Proc. Natl. Acad. Sci. U.S.A. 60, 668–674 - PMC - PubMed

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