Proteins > Glutamate receptor ionotropic, kainate 5
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Glutamate receptor ionotropic, kainate 5
A glutamate receptor ionotropic, kainate 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16478]
Synonyms
GluK5;
Excitatory amino acid receptor 2;
EAA2;
Glutamate receptor KA-2;
KA2
Research
Bioassay Publications (7)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 3 (42.86) | 18.2507 |
2000's | 4 (57.14) | 29.6817 |
2010's | 0 (0.00) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
Compounds (9)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
(S)-ATPA | Homo sapiens (human) | EC50 | 0.4800 | 1 | 1 |
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Enables
This protein enables 3 target(s):
Target | Category | Definition |
kainate selective glutamate receptor activity | molecular function | An ionotropic glutamate receptor activity that exhibits fast gating by glutamate, acts by opening a cation channel permeable to sodium and potassium, and for which kainate is an agonist. [GOC:mah, PMID:10049997, PMID:8804111] |
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential | molecular function | Any ligand-gated ion channel activity, occurring in the presynaptic membrane, that is involved in regulation of presynaptic membrane potential. [GOC:dos, PMID:15145529, PMID:19558451] |
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential | molecular function | Any transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
hippocampal mossy fiber to CA3 synapse | cellular component | One of the giant synapses that form between the mossy fiber axons of dentate gyrus granule cells and the large complex spines of CA3 pyramidal cells. It consists of a giant bouton known as the mossy fiber expansion, synapsed to the complex, multiheaded spine (thorny excresence) of a CA3 pyramidal cell. [DOI:10.1002/1096-9861, PMID:13869693, PMID:23264762] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
kainate selective glutamate receptor complex | cellular component | An assembly of four or five subunits which form a structure with an extracellular N-terminus and a large loop that together form the ligand binding domain. The C-terminus is intracellular. The ionotropic glutamate receptor complex itself acts as a ligand gated ion channel; on binding glutamate, charged ions pass through a channel in the center of the receptor complex. Kainate receptors are multimeric assemblies of GluK1-3 (also called GluR5-7), GluK4 (KA1) and GluK5 (KA2) subunits. [GOC:bf, http://www.bris.ac.uk/Depts/Synaptic/info/glutamate.html, PMID:18655795] |
Involved In
This protein is involved in 7 target(s):
Target | Category | Definition |
regulation of synaptic vesicle fusion to presynaptic active zone membrane | biological process | Any process that modulates the frequency, rate or extent of synaptic vesicle fusion to the presynaptic membrane. [GOC:mah] |
monoatomic ion transmembrane transport | biological process | A process in which a monoatomic ion is transported across a membrane. Monatomic ions (also called simple ions) are ions consisting of exactly one atom. [GOC:mah] |
ionotropic glutamate receptor signaling pathway | biological process | The series of molecular signals initiated by glutamate binding to a glutamate receptor on the surface of the target cell, followed by the movement of ions through a channel in the receptor complex, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, ISBN:0198506732] |
excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
regulation of presynaptic membrane potential | biological process | Any process that modulates the potential difference across a presynaptic membrane. [GOC:dph, GOC:ef] |
synaptic transmission, glutamatergic | biological process | The vesicular release of glutamate from a presynapse, across a chemical synapse, the subsequent activation of glutamate receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos] |
modulation of chemical synaptic transmission | biological process | Any process that modulates the frequency or amplitude of synaptic transmission, the process of communication from a neuron to a target (neuron, muscle, or secretory cell) across a synapse. Amplitude, in this case, refers to the change in postsynaptic membrane potential due to a single instance of synaptic transmission. [GOC:ai] |