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

Grik2 (P42260) - Overview - Molecular Target Synopsis

Protein


Grik2, Glutamate receptor ionotropic, kainate 2
UniProt P42260

Also Known as GRIK2_RAT, Grik2, Glur6

Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist (PubMed:17115050, PubMed:17486098). May be involved in the transmission of light information from the retina to the hypothalamus. Modulates cell surface expression of NETO2. Homotetramer or heterotetramer of pore-forming glutamate receptor subunits. Tetramers may be formed by the dimerization of dimers. Assembles into a kainate-gated homomeric channel that does not bind AMPA (By similarity). GRIK2 associated to GRIK5 forms functional channels that can be gated by AMPA. Interacts with DLG4. Interacts with NETO2. Interacts (via C-terminus) with KLHL17 (via kelch repeats); the interaction targets GRIK2 for degradation via ubiquitin-proteasome pathway.

5KUF
GLUK2EM WITH 2S,4R-4-METHYLGLUTAMATE
RCSB/PDB
Inspect Structure
See all 3D Structures for Grik2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
908P42260-1

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project Grik2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

RNA Interference


Grik2 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 Grik2 there are:
38 structures (98 chains) solved
37 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Grik2 has been screened with 673 compounds (974 bioactivities), 60 compounds have bioactivities that show binding affinity of <= 500nM (109 bioactivities). (see details)