Glutamate ionotropic receptor kainate type subunit 3 (GluK3) (GluK3)

Glutamate ionotropic receptor kainate type subunit 3 (GluK3) is a protein encoded by the GRIK3 gene that functions as a subunit of the ionotropic kainate-type glutamate receptor [1, 2]. It forms ligand-gated ion channels that are permeable to cations, primarily sodium and potassium, and sometimes calcium, mediating fast excitatory neurotransmission in the central nervous system [3, 11]. GluK3 is uniquely localized at both presynaptic and postsynaptic membranes, where it plays a critical role in modulating neurotransmitter release and regulating synaptic plasticity, particularly at hippocampal mossy fiber synapses [8, 13]. It is characterized by a relatively low affinity for glutamate and rapid desensitization compared to other kainate receptor subunits [12, 16]. Dysregulation or genetic variations in GluK3 have been linked to several neuropsychiatric and neurodevelopmental conditions, including schizophrenia, epilepsy, and developmental delay [2, 4, 5]. Additionally, aberrant expression of GluK3 has been observed in certain cancers, such as breast and colorectal cancer, where it may promote tumor progression [4, 6]. Pharmacological research has identified several agonists and antagonists, including selective compounds like Compound 28, which are being explored for their therapeutic potential in treating CNS disorders [8, 10].

Other names

GRIK3GLUR7GLR7EAA5Glutamate receptor ionotropic kainate 3GluR7aGluR7b

Agonism, competitive antagonism, and allosteric modulation of the ionotropic kainate receptor channel, which regulates cation influx and membrane depolarization [3, 8, 11, 17].