Target intelligence / Profile preview

Glutamate receptor ionotropic kainate 2 subunit (GluK2)

Target
GluK2
Molecular classification
Ion channel, Receptor, Ligand-gated ion channel, Ionotropic glutamate receptor, Kainate receptor
01

Overview

The **glutamate receptor ionotropic kainate 2 subunit** (commonly abbreviated GluK2, gene: GRIK2) is a protein that forms a core part of kainate-type ionotropic glutamate receptors, which are ligand-gated cation channels activated by the neurotransmitter glutamate and certain agonists such as kainic acid[1][2][3]. Kainate receptors are one of the three main classes of ionotropic glutamate receptors (along with AMPA and NMDA), and play key roles in *mediating excitatory synaptic transmission in the central nervous system*. The GluK2 subunit contributes to receptor diversity through alternative splicing and RNA editing, influencing channel properties, synaptic localization, and susceptibility to excitotoxicity. Functionally, these receptors participate in synaptic plasticity, regulation of neural circuits, learning, memory, and sensory processing (notably cold sensation)[2][3]. Mutations in GRIK2 are a known cause of certain neurodevelopmental disorders characterized by intellectual disability, language impairment, and seizures[1][2][4]. As a neuronal ion channel, GluK2 is a validated pharmacological and genetic target, though direct drugs are mostly for research or experimental use. Overactivation or dysfunction is associated with CNS toxicity and seizure risk, placing safety constraints on therapeutic modulation[1][3].

Other names
GluR6GLUR6Excitatory amino acid receptor 4 (EAA4)Glutamate receptor 6GRIK2
02

Mechanism of action

Agonists (e.g., kainic acid) activate the receptor leading to cation influx and neuronal excitation; antagonists would inhibit this excitatory transmission

03

Biological functions

Signal transductionChemical synaptic transmissionRegulation of membrane potentialExcitatory neurotransmissionSynaptic plasticityLearning and memoryVisual information processingCold sensation detection
04

Disease associations

Neurodevelopmental diseaseCognitive disabilityIntellectual developmental disorderPotential roles in other CNS/neuropsychiatric conditions
05

Safety considerations

CNS excitotoxicity if overactivatedrisk of seizuresneurodevelopmental side effects from antagonism or dysfunction
06

Interacting drugs

Kainic acid

2 more in the full profile.

07

Biomarkers

Mutations in GRIK2 for diagnosis of certain intellectual and neurodevelopmental disorderspotential biomarker status under investigation for epilepsy and neuropsychiatric conditions

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