A System for Assessing Dual Action Modulators of Glycine Transporters and Glycine Receptors.

Animals Biological Assay Gene Expression Glycine Plasma Membrane Transport Proteins / genetics Receptors, Glycine / genetics Synapses / metabolism Synaptic Transmission Xenopus laevis / genetics
analgesics glycine receptor glycine transporter lipids

Journal

Biomolecules
ISSN: 2218-273X
Titre abrégé: Biomolecules
Pays: Switzerland
ID NLM: 101596414

Informations de publication

Date de publication:
30 11 2020
Historique:
received: 23 10 2020
revised: 23 11 2020
accepted: 25 11 2020
entrez: 3 12 2020
pubmed: 4 12 2020
medline: 3 9 2021
Statut: epublish

Résumé

Reduced inhibitory glycinergic neurotransmission is implicated in a number of neurological conditions such as neuropathic pain, schizophrenia, epilepsy and hyperekplexia. Restoring glycinergic signalling may be an effective method of treating these pathologies. Glycine transporters (GlyTs) control synaptic and extra-synaptic glycine concentrations and slowing the reuptake of glycine using specific GlyT inhibitors will increase glycine extracellular concentrations and increase glycine receptor (GlyR) activation. Glycinergic neurotransmission can also be improved through positive allosteric modulation (PAM) of GlyRs. Despite efforts to manipulate this synapse, no therapeutics currently target it. We propose that dual action modulators of both GlyTs and GlyRs may show greater therapeutic potential than those targeting individual proteins. To show this, we have characterized a co-expression system in

Identifiants

DOI: 10.3390/biom10121618 PMID: 33266066 PMC: PMC7760315
pubmed: 33266066
pii: biom10121618
doi: 10.3390/biom10121618
pmc: PMC7760315
pii:
doi:

Substances chimiques

Glycine Plasma Membrane Transport Proteins 0
Receptors, Glycine 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : Australian NHMRC
ID : APP144429
Pays : International

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Auteurs

Diba Sheipouri (D)

School of Medical Sciences, University of Sydney, Sydney, NSW 2006, Australia.

Casey I Gallagher (CI)

School of Medical Sciences, University of Sydney, Sydney, NSW 2006, Australia.

Susan Shimmon (S)

School of Mathematical and Physical Sciences, University of Technology Sydney, Sydney, NSW 2007, Australia.

Tristan Rawling (T)

School of Mathematical and Physical Sciences, University of Technology Sydney, Sydney, NSW 2007, Australia.

Robert J Vandenberg (RJ)

School of Medical Sciences, University of Sydney, Sydney, NSW 2006, Australia.

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Classifications MeSH

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questionsmedicales.fr › Phénomènes génétiques › Expression des gènes › A System for Assessing Dual Action Modulators...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Transporteurs de neurotransmetteurs › Transporteurs plasmiques de neurotransmetteurs › Transporteurs de la glycine › A System for Assessing Dual Action Modulators...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteur de la glycine › A System for Assessing Dual Action Modulators...
questionsmedicales.fr › Cellules › Structures cellulaires › Membrane cellulaire › Structures de la membrane cellulaire › Jonctions intercellulaires › Synapses › A System for Assessing Dual Action Modulators...
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questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Amphibiens › Anura › Pipidae › Xenopus › Xenopus laevis › A System for Assessing Dual Action Modulators...