Glutamate receptor ionotropic, kainate 5 (GluK5) (GluK5)

Glutamate receptor ionotropic, kainate 5 (GluK5), also known as KA2, is a protein encoded by the GRIK5 gene that serves as a high-affinity subunit of the kainate-type ionotropic glutamate receptors (UniProt, Q16478). Unlike the GluK1-3 subunits, GluK5 is unable to form functional homomeric ion channels and must heteromerize with other subunits to produce functional receptors with distinct kinetic and pharmacological properties (Lerma & Marques, 2013, Neuron). These receptors are widely expressed throughout the central nervous system, particularly in the hippocampus and cerebral cortex, where they play a critical role in modulating excitatory synaptic transmission and plasticity (Contractor et al., 2011, Frontiers in Molecular Neuroscience). Dysregulation or genetic variations in GluK5 have been strongly linked to the pathophysiology of several neurological and psychiatric conditions, including temporal lobe epilepsy, schizophrenia, and bipolar disorder (Guan et al., 2016, Scientific Reports). Pharmacological targeting of GluK5-containing receptors offers a potential therapeutic avenue for managing neuronal hyperexcitability and cognitive deficits, although achieving high selectivity over other glutamate receptor subtypes remains a significant challenge (Jane et al., 2009, Molecular Pharmacology).

Other names

GRIK5KA2Glutamate receptor KA-2Excitatory amino acid receptor 2EAA2Ionotropic glutamate receptor type 5

Agonist or antagonist modulation of ionotropic glutamate signaling to regulate neuronal excitability and synaptic plasticity.