Glutamate receptor ionotropic kainate type subunit 5 (GluK5)

Glutamate receptor ionotropic kainate type subunit 5 (GluK5) is a protein encoded by the GRIK5 gene, forming part of the kainate receptor (KAR) family of ionotropic glutamate receptors. These receptors function as ligand-gated ion channels that mediate fast excitatory synaptic transmission in the central nervous system in response to glutamate binding. GluK5 is classified as a "high-affinity" KAR subunit and cannot form functional channels on its own; it must assemble into heteromeric complexes with other KAR subunits, notably GluK1, GluK2, or GluK3. Kainate receptors, including complexes containing GluK5, are present both pre- and post-synaptically, modulating neurotransmitter release and neuronal excitability. Genetic, structural, and pharmacological studies have associated aberrant KAR signaling and GluK5 function with epilepsy, schizophrenia, neurodegeneration, and other CNS pathologies. Although selective modulators for GluK5 are limited, the subunit remains a key research target for developing future treatments for neurological and psychiatric diseases.

Other names

GRIK5Glutamate receptor KA-2KA2Excitatory amino acid receptor 2 (EAA2)GluK5 subunitKainate receptor subunit KA2

Ligand-gated ion channel modulation: Drugs bind to the receptor and either activate (agonists) or inhibit (antagonists) its function, affecting cation permeability and synaptic potentials. Modulation of neurotransmission: By influencing excitatory synaptic currents and circuit modulation in the CNS. Partial agonism: Drugs like AMPA can produce partial activation by distinct binding domain conformational changes.