Target intelligence / Profile preview

Kainate receptor subunit 5 (GluK5)

Target
GluK5
Molecular classification
Ion channel, Receptor, Ionotropic glutamate receptor, Ligand-gated ion channel
01

Overview

Kainate receptor subunit 5 (GluK5, previously known as KA2, gene name GRIK5) is a protein that forms part of the kainate receptor family, which belongs to the ionotropic glutamate receptor superfamily of ligand-gated ion channels[1][6]. These receptors mediate excitatory synaptic transmission in the central nervous system by responding to the neurotransmitter glutamate. GluK5 does not form functional homomeric receptors but combines with other subunits (notably GluK1-3) to create functional heteromeric channels, most commonly as heterodimers with GluK2[2][3][5]. Kainate receptors, including complexes involving GluK5, are important for modulating synaptic strength and plasticity, contribute to neuronal circuit function, and are implicated in several neurological and neurodegenerative diseases. Their precise subunit composition determines their biophysical and pharmacological properties. Pharmacological targeting of kainate receptors is an<seg_64>area of ongoing research; however, there are currently no GluK5-selective drugs in clinical use[1][5][6].

Other names
GluK5KA2GRIK5 (gene name)Kainate-selective glutamate receptor subunit 5
02

Mechanism of action

Agonists: Bind and activate the receptor, increasing cation flux, leading to neuronal depolarization Antagonists: Bind and block the receptor, inhibiting excitatory neurotransmission mediated by kainate receptors

03

Biological functions

Signal transductionMediation of excitatory neurotransmissionModulation of synaptic transmissionRegulation of neuronal circuit activity
04

Disease associations

Neurodegenerative diseaseNeurological disorder (including epilepsy, schizophrenia, Alzheimer’s, depression)(Broad implication for diseases involving glutamatergic signaling)
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Safety considerations

Overactivation may contribute to excitotoxicity and neuronal cell deathTarget engagement in the CNS may lead to adverse neuropsychiatric or cognitive effectsSeizure risk due to altered glutamatergic transmission
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Interacting drugs

Kainic acid (agonist)

3 more in the full profile.

07

Biomarkers

Null (no clinically validated biomarkers for patient selection or efficacy monitoring specific to GluK5/Kainate receptor subunit 5)

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