GRIK1 Membrane Protein Introduction

Introduction of GRIK1

Glutamate receptors are the predominant excitatory neurotransmitter receptors in the mammalian brain and are divided into two classes: ionotropic glutamate receptors (iGluRs) and metabotropic glutamate receptors (mGluRs). Glutamate receptor ionotropic, kainate 1 (GluK1 or GRIK1) belongs to the kainate receptor (KAR) subfamily of iGluRs. KARs occur predominantly as homomeric or heteromeric combinations of GRIK1 and GRIK2 or as heteromers of these subunits with GRIK4 or GRIK5 subunits. This receptor is widely expressed in the central nervous system but is most abundant in the cerebellum and the suprachiasmatic nuclei of the hypothalamus. By binding to the excitatory neurotransmitter L-glutamate, a conformation change is induced, leading to the opening of the cation channel and the conversion of the chemical signal to an electrical impulse. Studies in various brain regions have demonstrated that GRIK1 KARs contributes to postsynaptic excitation of principal neurons and interneurons, and also act presynaptically to modulate GABA and glutamate release.

Basic Information of GRIK1
Protein Name Glutamate receptor ionotropic, kainate 1
Gene Name GRIK1
Aliases EAA3, GluR-5
Organism Homo sapiens (Human)
UniProt ID P39086
Transmembrane Times 3
Length (aa) 918

Functions of GRIK1 Membrane Protein

GRIK1 may be involved in the transmission of light information from the retina to the hypothalamus. Moreover, evidence has been provided that KARs primarily comprised of the GRIK1 subunit are important in transmission in nociceptive pathways, particularly in the context of persistent pain states. They have been identified in key brain areas involved in migraine pathophysiology. Additionally, studies have reported that the GRIK1 KARs could play a role in the pathophysiology of certain forms of epilepsy. With respect to therapeutic indications, antagonists for GRIK1 have shown positive activity in animal models of pain, migraine, epilepsy, stroke, and anxiety. Over the last decade, subunit selective agonists (e.g., ATPA and 5-iodowillardiine) and orthosteric (e.g., LY382884 and ACET) and allosteric antagonists for GRIK1 KARs have been developed.

GRIK1 Membrane Protein Introduction Application of GRIK1 Membrane Protein in Literature

  1. Sheng N., et al. Neto auxiliary proteins control both the trafficking and biophysical properties of the kainate receptor GluK1. Elife. 2015, 4. PubMed ID: 26720915

    This article investigated the role of Neto proteins, auxiliary subunits for KARs, in the synaptic trafficking of KAR GluK1. The results showed that Neto proteins played a critical role in controlling KARs properties and synaptic incorporation.

  2. Fritsch B., et al. Role of GluK1 kainate receptors in seizures, epileptic discharges, and epileptogenesis. Journal of Neuroscience. 2014, 34(17): 5765-5775. PubMed ID: 24760837

    This study used a potent and selective agonist GluK1 KARs and mice that are deficient in GluK1 and GluK2 to assess the role of GluK1 KARs in provoking seizures and in kindling epileptogenesis. The results showed that selective activation of GluK1 KARs can trigger seizures, but these receptors are not necessary for seizure generation in these models.

  3. Andreou A.P., et al. Modulation of nociceptive dural input to the trigeminocervical complex through GluK1 kainate receptors. Pain. 2015, 156(3): 439. PubMed ID: 25679470

    This study demonstrated a differential role of GluK1 receptors in the trigeminocervical complex (TCC), antagonism of which with antagonists can inhibit trigeminovascular activation through postsynaptic mechanisms.

  4. Sköld N., et al. Design, synthesis and in vitro pharmacology of GluK1 and GluK3 antagonists. Studies towards the design of subtype-selective antagonists through 2-carboxyethyl-phenylalanines with substituents interacting with non-conserved residues in the GluK binding sites. Bioorganic & medicinal chemistry. 2014, 22(19): 5368-5377. PubMed ID: 25172149

    This article reported the design, synthesis, and evaluation of in vitro pharmacology of antagonists selective for GluK1 and GluK3 KARs.

  5. Kaczor A.A., et al. Structural studies, homology modeling and molecular docking of novel non-competitive antagonists of GluK1/GluK2 receptors. Bioorganic & medicinal chemistry. 2014, 22(2): 787-795. PubMed ID: 24368028

    This article investigated the structure of novel indole-derived non-competitive antagonists of GluK1/GluK2 receptors using techniques such as X-ray structure determination, NMR and MS spectra. Besides, homology modeling and molecular blocking were also studied.

GRIK1 Preparation Options

Many of the molecular mechanisms and physiological functions of GRIK1 remain to be elucidated in the future. To facilitate the studies of this membrane protein, Creative Biolabs now provides membrane protein preparation services using various strategies and approaches. Besides, we are also experienced in dealing with other membrane protein targets, covering G-protein coupled membrane proteins, ion channels, and other transporters. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-GRIK1 antibody development services.

As an industry leader in the field of membrane protein production and antibody development, Creative Biolabs combines our advanced proteomic technologies and our long-term scientific expertise in membrane biochemistry to provide our clients with the best quality services with reasonable prices. Contact us if you want to know more about our membrane protein preparation services.

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