PMID: 9159229Sep 1, 1996Paper

Molecular biology of the GABA(A) receptor: functional domains implicated by mutational analysis

Frontiers in Bioscience : a Journal and Virtual Library
M DaviesS M Dunn

Abstract

GABA(A) receptors are the major inhibitory neurotransmitter receptors in mammalian brain. They belong to a family of ligand-gated ion channels that also includes the nicotinic acetylcholine receptors, glycine receptors and 5HT(3) receptors. Each receptor in the family is believed to be a pentamer of homologous subunits that assemble to form a central transmembrane ion pore which, in the case of the GABA(A) receptor, is anion-selective. For almost twenty years, there has been tremendous interest in the structure and function of GABA(A) receptors, not only because of their importance in regulating brain excitability but also because these proteins are the specific targets for a wide variety of therapeutic agents including the anxiolytic benzodiazepines and barbiturates. Molecular cloning has revealed that GABA(A) receptors are heterogeneous, being formed by combinations of different isoforms of several subunit classes (alpha, beta, gamma, delta). The physiological and pharmacological properties of individual GABAA receptor subtypes appear to depend on their precise subunit complement. In this review, we focus on the application of modern techniques in molecular biology, particularly mutational analysis, to identify structural dom...Continue Reading

Citations

Mar 1, 2012·Archives of Pharmacal Research·Jae-Wook KimKi-Wan Oh
Jun 26, 2014·Experimental Neurobiology·Junsung WooC Justin Lee
Jun 18, 2019·Chemical Biology & Drug Design·Zuleyma Martínez-CamposRodrigo Said Razo-Hernández

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