kainate selective glutamate receptor activity
Definition
Target type: molecularfunction
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]
Kainate selective glutamate receptor activity is a molecular function that describes the binding and activation of kainate receptors, a subtype of ionotropic glutamate receptors. These receptors are integral membrane proteins that mediate excitatory synaptic transmission in the central nervous system. Kainate receptors are permeable to sodium, potassium, and calcium ions, and their activation leads to depolarization of the postsynaptic membrane.
The molecular mechanism of kainate receptor activation involves the binding of glutamate to the receptor's extracellular domain. This binding event triggers a conformational change in the receptor, which opens the ion channel and allows the passage of ions. The specific sequence of events involved in this process is still being investigated.
Kainate receptors are known to play a role in a variety of neuronal functions, including synaptic plasticity, learning, and memory. They are also implicated in several neurological disorders, such as epilepsy, stroke, and Alzheimer's disease. The specific role of kainate receptors in these disorders is complex and not fully understood.
Kainate receptors are found in various brain regions, including the hippocampus, cortex, and cerebellum. They are expressed in both excitatory and inhibitory neurons, and they can be either presynaptic or postsynaptic. The diverse distribution and function of kainate receptors highlight their importance in neuronal signaling and plasticity.
Furthermore, the specific molecular function of kainate receptors is influenced by their subunit composition. Kainate receptors are heteromeric proteins composed of different subunits, each contributing to the receptor's pharmacological properties and functional characteristics. The diversity of subunit combinations allows for a fine-tuning of kainate receptor activity in different neuronal circuits.'
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Proteins (5)
| Protein | Definition | Taxonomy |
|---|---|---|
| Glutamate receptor ionotropic, kainate 4 | A glutamate receptor ionotropic, kainate 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16099] | Homo sapiens (human) |
| Glutamate receptor ionotropic, kainate 5 | A glutamate receptor ionotropic, kainate 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16478] | Homo sapiens (human) |
| Glutamate receptor ionotropic, kainate 3 | A glutamate receptor ionotropic, kainate 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13003] | Homo sapiens (human) |
| Glutamate receptor ionotropic, kainate 2 | A glutamate receptor ionotropic, kainate 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13002] | Homo sapiens (human) |
| Glutamate receptor ionotropic, kainate 1 | A glutamate receptor ionotropic, kainate 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P39086] | Homo sapiens (human) |
Compounds (20)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid: An IBOTENIC ACID homolog and glutamate agonist. The compound is the defining agonist for the AMPA subtype of glutamate receptors (RECEPTORS, AMPA). It has been used as a radionuclide imaging agent but is more commonly used as an experimental tool in cell biological studies. | non-proteinogenic alpha-amino acid | |
| kainic acid | Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose. | dicarboxylic acid; L-proline derivative; non-proteinogenic L-alpha-amino acid; pyrrolidinecarboxylic acid | antinematodal drug; excitatory amino acid agonist |
| glutamic acid | glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2. Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM. | glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical |
| sym 2081 | |||
| 5-fluorowillardiine | 3-(5-fluorouracil-1-yl)-L-alanine : An alanine derivative that is L-alanine bearing a 5-fluorouracil-1-yl substituent at position 3. A more potent and selective AMPA receptor agonist (at hGluR1 and hGluR2) than AMPA itself (Ki = 14.7, 25.1, and 1820 nM for hGluR1, hGluR2 and hGluR5 respectively). 5-fluorowillardiine: a glutamate agonist; RN given for (S)-isomer | L-alanine derivative; non-proteinogenic L-alpha-amino acid; organofluorine compound | AMPA receptor agonist |
| ly 293558 | tezampanel: structure given in first source; an AMPA receptor antagonist | ||
| ns 1608 | NS 1608: a BK(Ca) channel opener | ureas | |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | |||
| 5-bromowillardiine | 5-bromowillardiine: acts as a kainate-like agonist on chick EAA receptors expressed in Xenopus oocytes; RN given refers to (S)-isomer; RN for cpd without isomeric designation not avail 5/91 | ||
| willardiine | 3-(uracil-1-yl)-L-alanine : The 3-(uracil-1-yl) derivative of L-alanine. willardiine: isolated from seeds of Acacia willariana; structure | amino acid zwitterion; L-alanine derivative; non-proteinogenic L-alpha-amino acid | |
| (S)-ATPA | (S)-ATPA : A non-proteinogenic L-alpha-amino acid that is L-alanine in which one of the methyl hydrogens is replaced by a 5-tert-butyl-3-hydroxy-isooxazol-4-yl group. | isoxazoles; non-proteinogenic L-alpha-amino acid | metabolite |
| ly382884 | benzoic acids | ||
| 4-bromohomoibotenic acid, (rs)-isomer | |||
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline: structure given in first source; neuroprotectant for cerebral ischemia; AMPA receptor antagonist | naphthalenes; sulfonic acid derivative | |
| ubp 310 | UBP 310: a GluR5 antagonist; structure in first source | ||
| ubp 302 | |||
| dysiherbaine | dysiherbaine : A furopyran that is (3aR,7aR)-hexahydro-2H-furo[3,2-b]pyran substituted by carboxy, (2S)-2-amino-2-carboxyethyl, hydroxy and methylamino groups at positions 2, 2, 6, and 7, respectively (the 2R,3aR,6S,7R,7aR-stereoisomer). A convulsant isolated from the marine sponge Dysidea herbacea that has high affinity for kainate ionotropic glutamate receptors. dysiherbaine: an exitotoxic amino acid; structure in first source | amino dicarboxylic acid; furopyran; hydroxy carboxylic acid; secondary amino compound | animal metabolite; excitatory amino acid agonist; marine metabolite; neurotoxin |
| ns 1652 | NS 1652: an anion conductance inhibitor; structure in first source | ||
| ns3694 | NS3694: an apoptosome inhibitor | ureas | |
| ubp296 | UBP296: potent and selective kainate receptor antagonist; structure in first source | alpha-amino acid |