Mutation of An Arginine Residue in the Human Glycine Receptor Transforms Beta-Alanine and Taurine From Agonists Into Competitive Antagonists

Rajendra, S, Lynch, JW, Pierce, KD, French, CR, Barry, PH and Schofield, PR (1995) Mutation of An Arginine Residue in the Human Glycine Receptor Transforms Beta-Alanine and Taurine From Agonists Into Competitive Antagonists. Neuron, 14 1: 169-175. doi:10.1016/0896-6273(95)90251-1


Author Rajendra, S
Lynch, JW
Pierce, KD
French, CR
Barry, PH
Schofield, PR
Title Mutation of An Arginine Residue in the Human Glycine Receptor Transforms Beta-Alanine and Taurine From Agonists Into Competitive Antagonists
Journal name Neuron   Check publisher's open access policy
ISSN 0896-6273
Publication date 1995-01-01
Year available 1995
Sub-type Article (original research)
DOI 10.1016/0896-6273(95)90251-1
Open Access Status DOI
Volume 14
Issue 1
Start page 169
End page 175
Total pages 7
Place of publication CAMBRIDGE
Publisher CELL PRESS
Language eng
Abstract Agonist binding to the inhibitory glycine receptor (GlyR) initiates the opening of a chloride-selective channel that modulates the neuronal membrane potential. Point mutations of the GlyR, substituting Arg-271 with either Leu or Gin, have been shown to underlie the inherited neurological disorder startle disease (hyperekplexia). We show that these substitutions result in the redistribution of GlyR single-channel conductances to lower conductance levels. Additionally, the binding of the glycinergic agonists beta-alanine and taurine to mutated GryRs does not initiate a chloride current, but instead competitively antagonizes currents activated by glycine. These findings are consistent with mutations of Arg-271 resulting in the uncoupling of the agonist binding process from the channel activation mechanism of the receptor.
Keyword Nicotinic Acetylcholine-Receptor
Functional Expression
Ion Channel
Binding Sites
Subunit
Pharmacology
Cells
Activation
Conductance
Resolution
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: ResearcherID Downloads - Archived
 
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