Introduction of GRIK5
Glutamate receptor ionotropic, kainate 5 (GRIK5) is a protein that in humans is encoded by the GRIK5 gene. This protein belongs to the glutamate-gated ionic channel family, termed ionotropic glutamate receptors (iGluRs). AMPA, NMDA, and kainate receptors (KARs) are the three main types of iGluRs and they are composed of distinct subunit populations. The tetrameric KARs can be assembled from five different subunits (GRIK1-GRIK5). GRIK5 is widely distributed throughout the central nervous system including the hippocampus, cortex, and the granule cell layer of the cerebellum. Unlike the "low-affinity" GRIK1-3 subunits that are able to produce functional homomeric receptors by themselves, the "high-affinity" GRIK4 and GRIK5 subunits associate with GRIK1, 2, or 3 to form functional channels. GRIK5, in heteromeric complexes with GRIK2, constitutes the most abundant KAR subtypes in the brain.
|Basic Information of GRIK5|
|Protein Name||Glutamate receptor ionotropic, kainate 5|
|Organism||Homo sapiens (Human)|
Functions of GRIK5 Membrane Protein
As one subunit of the KARs, GRIK5 proteins are involved in the regulation of neurotransmitter release, circuit modulation, and neuronal excitability. Moreover, some studies have indicated that GRIK5 is associated with various diseases in the central nervous system (e.g. schizophrenia, temporal lobe epilepsy, bipolar disorder), selective GRIK5 ligands could have therapeutic potential. Among the current agonists and antagonists for KARs, AMPA, ATPA and (S)-5-iodowillardiine can function as partial agonists of GluR6/KA2 heteromeric receptors. Studies have proposed that the future development of selective antagonists (such as non-competitive ligands) for the major subtype of KAR in the brain, composed of GRIK2 and GRIK5, will be extremely useful.
Fig.1 Scheme of kainite receptor subunits. (Pinheiro, 2006)
Application of GRIK5 Membrane Protein in Literature
This article reported a pharmacological profile of the GluK5 kainate receptor using 27 ligands. The pharmacological profile of GluK5 is distinct from that of the other kainate receptors (GluK1-3). The results suggested that selective ligands of GluK5 could be designed for therapeutic purposes.
This article reported that repeated pairing of pre- and postsynaptic stimulation at hippocampal mossy fiber synapses induced long-term depression of kainate receptor (KAR)-mediated responses, which depends on Ca(2+) influx, activation of CaMKII, and on the GluK5 subunit of KARs.
This study investigated the stoichiometry of the full-length GluK2/GluK5 complex receptor, using a single-molecule imaging technique. The results showed that GluK2 and GluK5 assembled with 2:2 stoichiometry, forming a heterotetramer.
This article examined the relative importance of occupancy of the agonist site of the GluK2 or GluK5 subunit for surface expression of heteromeric receptors. The results showed that ligand binding to only the GluK5 subunit was necessary and sufficient to allow trafficking of the recombinant heteromer to the cell membrane, but that occupancy of the GluK2 site was not.
This study described new properties associated with domoate (an agonist at kainite-type receptors) action at kainite receptors and further characterized the distinct roles played by different subunits in GluK2/GluK5 heteromeric receptors.
GRIK5 Preparation Options
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