Tclin GRIN2B Glutamate receptor ionotropic, NMDA 2B

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:28126851). Sensitivity to glutamate and channel kinetics depend on the subunit composition (PubMed:8768735, PubMed:26875626). In concert with DAPK1 at extrasynaptic sites, acts as a central mediator for stroke damage. Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them, resulting in an irreversible neuronal death. Contributes to neural pattern formation in the developing brain. Plays a role in long-term depression (LTD) of hippocampus membrane currents and in synaptic plasticity (By similarity). This gene encodes a member of the N-methyl-D-aspartate (NMDA) receptor family within the ionotropic glutamate receptor superfamily. The encoded protein is a subunit of the NMDA receptor ion channel which acts as an agonist binding site for glutamate. The NMDA receptors mediate a slow calcium-permeable component of excitatory synaptic transmission in the central nervous system. The NMDA receptors are heterotetramers of seven genetically encoded, differentially expressed subunits including NR1 (GRIN1), NR2 (GRIN2A, GRIN2B, GRIN2C, or GRIN2D) and NR3 (GRIN3A or GRIN3B). The early expression of this gene in development suggests a role in brain development, circuit formation, synaptic plasticity, and cellular migration and differentiation. Naturally occurring mutations within this gene are associated with neurodevelopmental disorders including autism spectrum disorder, attention deficit hyperactivity disorder, epilepsy, and schizophrenia. [provided by RefSeq, Aug 2017]

Uniprot Accession IDs

• Q13224
• Q12919
• Q13220
• Q13225
• Q14CU4
• Q9UM56
• GluN2B

Gene Name

• GRIN2B

Ensembl ID

• ENST00000609686
• ENSP00000477455
• ENSG00000273079

Symbol

• NMDAR2B
• NR3
• MRD6
• NR2B
• hNR3
• EIEE27
• GluN2B
• NMDAR2B

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
hub protein	1
molecular function	1
trait	1
ligand (chemical)	0.94
biological term	0.92

Protein Classes

DTO Classes

Protein / Ion Channel / Glutamate-gated Ion Channel (Gic) Family Of Neurotransmitter Receptors / Nr2b/grin2b Subfamily / Glutamate Receptor Ionotropic, Nmda 2b

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: 3374.05   (req: < 5)

Gene RIFs: 209   (req: <= 3)

Antibodies: 1245   (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: 3374.05   (req: >= 5)

Gene RIFs: 209   (req: > 3)

Antibodies: 1245   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 23

Tchem

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

Active Ligands: 216

Tclin

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

Active Drugs: 5