Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. (Q46100388)

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scientific article published in January 2013

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English	Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain.	scientific article published in January 2013

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scholarly article

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22 February 2020

Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain (English)

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22 February 2020

allosteric inhibitor

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Christoph Fahlke

5

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22 February 2020

Anders A Jensen

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22 February 2020

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22 February 2020

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Bjarke Abrahamsen

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22 February 2020

Nicole Schneider

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22 February 2020

Mette N Erichsen

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22 February 2020

Tri H V Huynh

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1 January 2013

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22 February 2020

Journal of Neuroscience

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22 February 2020

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22 February 2020

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22 February 2020

1068-1087

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22 February 2020

Glutamate release in severe brain ischaemia is mainly by reversed uptake.

1 reference

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12 December 2020

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Arginine 447 plays a pivotal role in substrate interactions in a neuronal glutamate transporter

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https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Glutamate uptake

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https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists

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Agonist- and antagonist-induced sequestration/internalization of neuropeptide Y Y1 receptors in HEK293 cells

1 reference

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12 December 2020

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A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

1 reference

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12 December 2020

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Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine

1 reference

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12 December 2020

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Glutamate modifies ion conduction and voltage-dependent gating of excitatory amino acid transporter-associated anion channels

1 reference

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12 December 2020

based on heuristic

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The chloride permeation pathway of a glutamate transporter and its proximity to the glutamate translocation pathway.

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Glutamate transporters: animal models to neurologic disease

1 reference

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12 December 2020

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Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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A trimeric quaternary structure is conserved in bacterial and human glutamate transporters

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

based on heuristic

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Allosteric modulation of neurotransmitter transporters at excitatory synapses.

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Structure of a glutamate transporter homologue from Pyrococcus horikoshii

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

based on heuristic

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Small-scale molecular motions accomplish glutamate uptake in human glutamate transporters

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Individual subunits of the glutamate transporter EAAC1 homotrimer function independently of each other

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors

1 reference

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12 December 2020

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Coupling substrate and ion binding to extracellular gate of a sodium-dependent aspartate transporter

1 reference

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12 December 2020

based on heuristic

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The glutamate and chloride permeation pathways are colocalized in individual neuronal glutamate transporter subunits

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Aspartate-444 is essential for productive substrate interactions in a neuronal glutamate transporter

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

based on heuristic

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Mutations in transmembrane domains 5 and 7 of the human excitatory amino acid transporter 1 affect the substrate-activated anion channel.

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Glutamate excitotoxicity and therapeutic targets for amyotrophic lateral sclerosis.

1 reference

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12 December 2020

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High-frequency HTR3B variant associated with major depression dramatically augments the signaling of the human 5-HT3AB receptor

1 reference

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12 December 2020

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Antidepressant-induced internalization of the serotonin transporter in serotonergic neurons

1 reference

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12 December 2020

based on heuristic

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Sodium-coupled neurotransmitter transporters

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1

1 reference

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12 December 2020

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The four major N- and C-terminal splice variants of the excitatory amino acid transporter GLT-1 form cell surface homomeric and heteromeric assemblies.

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Excitatory amino acid transporters as potential drug targets.

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Current approaches with the glutamatergic system as targets in the treatment of neuropathic pain

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12 December 2020

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Glutamate receptors as therapeutic targets for Parkinson's disease

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Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function

1 reference

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12 December 2020

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Transport mechanism of a bacterial homologue of glutamate transporters.

1 reference

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12 December 2020

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Antagonists and substrates differentially regulate serotonin transporter cell surface expression in serotonergic neurons

1 reference

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12 December 2020

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Structural perspectives on secondary active transporters.

1 reference

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New views of glutamate transporter structure and function: advances and challenges.

1 reference

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12 December 2020

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Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101).

1 reference

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Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators

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SLC6 neurotransmitter transporters: structure, function, and regulation

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Allosteric modulation of metabotropic glutamate receptors

1 reference

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Targeting glutamate synapses in schizophrenia

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Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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inferred from PubMed ID database lookup

Transient striatal GLT-1 blockade increases EAAC1 expression, glutamate reuptake, and decreases tyrosine hydroxylase phosphorylation at ser(19).

1 reference

https://pubmed.ncbi.nlm.nih.gov/23325245

12 December 2020

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Crystal structure of an asymmetric trimer of a bacterial glutamate transporter homolog

1 reference

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Glutamatergic neurotransmission as molecular target of new anticonvulsants

1 reference

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12 December 2020

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Activation of glutamate transport evokes rapid glutamine release from perisynaptic astrocytes

1 reference

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12 December 2020

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Neutralizing aspartate 83 modifies substrate translocation of excitatory amino acid transporter 3 (EAAT3) glutamate transporters.

1 reference

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12 December 2020

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Alterations of gene expression and glutamate clearance in astrocytes derived from an MeCP2-null mouse model of Rett syndrome

1 reference

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12 December 2020

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inferred from PubMed ID database lookup

Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configuratio

1 reference

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12 December 2020

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inferred from PubMed ID database lookup

GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes

1 reference

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12 December 2020

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The glutamate aspartate transporter (GLAST) mediates L-glutamate-stimulated ascorbate-release via swelling-activated anion channels in cultured neonatal rodent astrocytes.

1 reference

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Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102.

1 reference

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1 reference

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Engineering hybrid genes without the use of restriction enzymes: gene splicing by overlap extension

1 reference

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Ion fluxes associated with excitatory amino acid transport.

1 reference

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12 December 2020

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Functional analysis of the high affinity, Na(+)-dependent glutamate transporter GLAST-1 by site-directed mutagenesis

1 reference

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12 December 2020

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An excitatory amino-acid transporter with properties of a ligand-gated chloride channel

1 reference

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12 December 2020

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The Cheng-Prusoff relationship: something lost in the translation.

1 reference

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Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor

1 reference

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12 December 2020

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DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters

1 reference

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12 December 2020

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Identification of functional domains of the human glutamate transporters EAAT1 and EAAT2.

1 reference

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12 December 2020

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inferred from PubMed ID database lookup

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10.1523/JNEUROSCI.3396-12.2013

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22 February 2020

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22 February 2020

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22 February 2020

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