Tclin GRIN2A Glutamate receptor ionotropic, NMDA 2A

Protein Summary

Description

Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:8768735, PubMed:26919761, PubMed:26875626, PubMed:28105280). Sensitivity to glutamate and channel kinetics depend on the subunit composition; channels containing GRIN1 and GRIN2A have higher sensitivity to glutamate and faster kinetics than channels formed by GRIN1 and GRIN2B (PubMed:26919761, PubMed:26875626). Contributes to the slow phase of excitatory postsynaptic current, long-term synaptic potentiation, and learning (By similarity). This gene encodes a member of the glutamate-gated ion channel protein family. The encoded protein is an N-methyl-D-aspartate (NMDA) receptor subunit. NMDA receptors are both ligand-gated and voltage-dependent, and are involved in long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning. These receptors are permeable to calcium ions, and activation results in a calcium influx into post-synaptic cells, which results in the activation of several signaling cascades. Disruption of this gene is associated with focal epilepsy and speech disorder with or without cognitive disability. Alternative splicing results in multiple transcript variants. [provided by RefSeq, May 2014]

Uniprot Accession IDs

• Q12879
• O00669
• Q17RZ6
• GluN2A

Gene Name

• GRIN2A

Ensembl ID

• ENST00000330684
• ENSP00000332549
• ENSG00000183454
• ENST00000396573
• ENSP00000379818
• ENST00000562109
• ENSP00000454998

Symbol

• NMDAR2A
• LKS
• EPND
• FESD
• NR2A
• GluN2A
• NMDAR2A

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	0.99
trait	0.97
ligand (chemical)	0.94
biological process	0.86
gene perturbation	0.86

Protein Classes

DTO Classes

Protein / Ion Channel / Glutamate-gated Ion Channel (Gic) Family Of Neurotransmitter Receptors / Nr2a/grin2a Subfamily / Glutamate Receptor Ionotropic, Nmda 2a

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: 1762.29   (req: < 5)

Gene RIFs: 118   (req: <= 3)

Antibodies: 715   (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: 1762.29   (req: >= 5)

Gene RIFs: 118   (req: > 3)

Antibodies: 715   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 32

Tchem

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

Active Ligands: 9

Tclin

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

Active Drugs: 5