ArticleThe Journal of biological chemistry2010
Identification of novel specific allosteric modulators of the glycine receptor using phage display.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 30 citations in OpenAlex.
- A System for Assessing Dual Action Modulators of Glycine Transporters and Glycine Receptors.Biomolecules · 2020Article
- A Novel Peptide Restricts Ethanol Modulation of the BK Channel In Vitro and In Vivo.The Journal of pharmacology and experimental therapeutics · 2018Article
- Application of phage peptide display technology for the study of food allergen epitopes.Molecular nutrition & food research · 2017Review
- Identification and characterization of heptapeptide modulators of the glycine receptor.European journal of pharmacology · 2016Article
- Allosteric modulation of the glycine receptor activated by agonists differing in efficacy.Brain research · 2015Article
- Generation of recombinant antibodies to rat GABAA receptor subunits by affinity selection on synthetic peptides.PloS one · 2014Article
- Contaminating levels of zinc found in commonly-used labware and buffers affect glycine receptor currents.Brain research bulletin · 2014Article
- Physiological concentrations of zinc reduce taurine-activated GlyR responses to drugs of abuse.Neuropharmacology · 2013Article
- Trifluoroacetate is an allosteric modulator with selective actions at the glycine receptor.Neuropharmacology · 2012Article
- Allosteric modulation of glycine receptors.British journal of pharmacology · 2011Review
- Generation of recombinant guinea pig antibody fragments to the human GABAC receptor.Journal of immunological methods · 2011Article
- Peptide phage display as a tool for drug discovery: targeting membrane receptors.Molecules (Basel, Switzerland) · 2011Review
- Phage display: selecting straws instead of a needle from a haystack.Molecules (Basel, Switzerland) · 2011Review
- Mechanism of Allosteric Modulation of the Cys-loop Receptors.Pharmaceuticals (Basel, Switzerland) · 2010Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The glycine receptor (GlyR) is a member of the Cys-loop superfamily of ligand-gated ion channels and the major mediator of inhibitory neurotransmission in the spinal cord and brainstem. Many allosteric modulators affect the functioning of members of this superfamily, with some such as benzodiazepines showing great specificity and others such as zinc, alcohols, and volatile anesthetics acting on multiple members. To date, no potent and efficacious allosteric modulator acting specifically at the GlyR has been identified, hindering both experimental characterization of the receptor and development of GlyR-related therapeutics. We used phage display to identify novel peptides that specifically modulate GlyR function. Peptide D12-116 markedly enhanced GlyR currents at low micromolar concentrations but had no effects on the closely related gamma-aminobutyric acid type A receptors. This approach can readily be adapted for use with other channels that currently lack specific allosteric modulators.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.