Hyperekplexia mutations of the glycine receptor unmask the inhibitory subsite for beta-amino-acids

Neuroreport
B LaubeV Schmieden

Abstract

beta-Alanine and taurine are agonists of the glycine receptor (GlyR) which, at low concentrations, antagonize the action of the principal agonist glycine. We analysed the potency of these ligands on alpha 1 subunits mutated at residue R271. GlyRs formed from alpha 1R271K subunits showed a reduction of beta-alanine and taurine affinities and maximal inducible currents; the mutants alpha 1R271Q and alpha 1R271L associated with human hyperekplexia gave no responses to these ligands. Inhibition of glycine-evoked currents by beta-alanine and taurine, however, was similar for all mutant GlyRs. These data are consistent with the existence of two subdomains within the ligand binding region of the GlyR, an agonistic one, which depends on arginine 271, and an antagonistic subsite, which is not connected to this residue.

Citations

Jan 1, 1997·Pharmacology & Therapeutics·S RajendraP R Schofield
Nov 24, 1999·Clinical and Experimental Pharmacology & Physiology·J W LynchP R Schofield
Jul 22, 1999·Annals of the New York Academy of Sciences·H BetzR J Harvey
Oct 16, 2014·BioMed Research International·Ahmed MaherHans-Georg Breitinger
Sep 24, 2004·Physiological Reviews·Joseph W Lynch
Aug 15, 2013·British Journal of Pharmacology·Natascha SchaeferCarmen Villmann
Mar 30, 2001·The Journal of Biological Chemistry·Q ShanJ W Lynch
Jul 17, 1998·Science·P JonasJ Sandkühler

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