Tclin GRIA2 Glutamate receptor 2

Protein Summary

Description

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. 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. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate. Through complex formation with NSG1, GRIP1 and STX12 controls the intracellular fate of AMPAR and the endosomal sorting of the GRIA2 subunit toward recycling and membrane targeting (By similarity). Glutamate receptors are the predominant excitatory neurotransmitter receptors in the mammalian brain and are activated in a variety of normal neurophysiologic processes. This gene product belongs to a family of glutamate receptors that are sensitive to alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA), and function as ligand-activated cation channels. These channels are assembled from 4 related subunits, GRIA1-4. The subunit encoded by this gene (GRIA2) is subject to RNA editing (CAG->CGG; Q->R) within the second transmembrane domain, which is thought to render the channel impermeable to Ca(2+). Human and animal studies suggest that pre-mRNA editing is essential for brain function, and defective GRIA2 RNA editing at the Q/R site may be relevant to amyotrophic lateral sclerosis (ALS) etiology. Alternative splicing, resulting in transcript variants encoding different isoforms, (including the flip and flop isoforms that vary in their signal transduction properties), has been noted for this gene. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P42262
• A8MT92
• I6L997
• Q96FP6
• GluR-2

Gene Name

• GRIA2

Ensembl ID

• ENST00000264426
• ENSP00000264426
• ENSG00000120251
• ENST00000296526
• ENSP00000296526
• ENST00000393815
• ENSP00000377403
• ENST00000507898
• ENSP00000426845
• ENST00000645636
• ENSP00000495569

Symbol

• GLUR2
• GLUR2
• GLURB
• GluA2
• HBGR2
• GluR-K2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
drug	0.99
molecular function	0.86
biological term	0.76
cellular component	0.76
disease perturbation	0.74

Protein Classes

DTO Classes

Protein / Ion Channel / Glutamate-gated Ion Channel (Gic) Family Of Neurotransmitter Receptors / Gria2 Subfamily / Glutamate Receptor 2

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 895.05   (req: < 5)

Gene RIFs: 63   (req: <= 3)

Antibodies: 597   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 895.05   (req: >= 5)

Gene RIFs: 63   (req: > 3)

Antibodies: 597   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 7

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 214

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 5