Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

Grik3 (P42264) - Overview - Molecular Target Synopsis

Protein


Grik3, Glutamate receptor ionotropic, kainate 3
UniProt P42264

Also Known as GRIK3_RAT, Grik3, Glur7

Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists. This receptor binds domoate > kainate >> L-glutamate = quisqualate >> AMPA = NMDA. Homotetramer, and heterotetramer with GRIK4 or GRIK5. Homomeric GLUR7A and GLUR7B form functional kainate receptors. GLUR7A receptors have a very low sensitivity to glutamate. GLUR7A can also coassemble with either GRIK4 or GRIK5 to form heteromeric receptors. Interacts with PRKCABP. Interacts with NETO2.

6F29
CRYSTAL STRUCTURE OF THE KAINATE RECEPTOR GLUK3 LIGAND BINDING DOMAIN IN COMPLEX WITH (S)-1-[2-AMINO-2-CARBOXYETHYL]-5,7-DIHYDROTHIENO[3,4- D]PYRIMIDIN-2,4(1H,3H)-DIONE AT RESOLUTION 2.6A
RCSB/PDB
Inspect Structure
See all 3D Structures for Grik3

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
919P42264-1
910P42264-2

Sub-cellular localization


UniProt: Grik3 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: Grik3 is active in the following subcellular-locations: axon, cell junction, dendrite, dendrite cytoplasm, kainate selective glutamate receptor complex, perikaryon, plasma membrane, postsynaptic membrane, presynaptic membrane, terminal bouton.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Grik3 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

RNA Interference


Grik3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: . (see details)

3D Structures


For Grik3 there are:
15 structures (25 chains) solved
15 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Grik3 has been screened with 581 compounds (868 bioactivities), 47 compounds have bioactivities that show binding affinity of <= 500nM (93 bioactivities). (see details)