General Information of the Protein
Protein ID |
PT02751
|
||||
---|---|---|---|---|---|
Protein Name |
Glutamate receptor ionotropic, NMDA 2B
|
||||
Secondarily Protein Name |
Glutamate [NMDA] receptor subunit epsilon-2
N-methyl D-aspartate receptor subtype 2B
N-methyl-D-aspartate receptor subunit 3
|
||||
Gene Name |
GRIN2B
|
||||
Secondarily Gene Name |
NMDAR2B
|
||||
Sequence |
MKPRAECCSPKFWLVLAVLAVSGSRARSQKSPPSIGIAVILVGTSDEVAIKDAHEKDDFHHLSVVPRVELVAMNETDPKSIITRICDLMSDRKIQGVVFADDTDQEAIAQILDFISAQTLTPILGIHGGSSMIMADKDESSMFFQFGPSIEQQASVMLNIMEEYDWYIFSIVTTYFPGYQDFVNKIRSTIENSFVGWELEEVLLLDMSLDDGDSKIQNQLKKLQSPIILLYCTKEEATYIFEVANSVGLTGYGYTWIVPSLVAGDTDTVPAEFPTGLISVSYDEWDYGLPARVRDGIAIITTAASDMLSEHSFIPEPKSSCYNTHEKRIYQSNMLNRYLINVTFEGRNLSFSEDGYQMHPKLVIILLNKERKWERVGKWKDKSLQMKYYVWPRMCPETEEQEDDHLSIVTLEEAPFVIVESVDPLSGTCMRNTVPCQKRIVTENKTDEEPGYIKKCCKGFCIDILKKISKSVKFTYDLYLVTNGKHGKKINGTWNGMIGEVVMKRAYMAVGSLTINEERSEVVDFSVPFIETGISVMVSRSNGTVSPSAFLEPFSADVWVMMFVMLLIVSAVAVFVFEYFSPVGYNRCLADGREPGGPSFTIGKAIWLLWGLVFNNSVPVQNPKGTTSKIMVSVWAFFAVIFLASYTANLAAFMIQEEYVDQVSGLSDKKFQRPNDFSPPFRFGTVPNGSTERNIRNNYAEMHAYMGKFNQRGVDDALLSLKTGKLDAFIYDAAVLNYMAGRDEGCKLVTIGSGKVFASTGYGIAIQKDSGWKRQVDLAILQLFGDGEMEELEALWLTGICHNEKNEVMSSQLDIDNMAGVFYMLGAAMALSLITFICEHLFYWQFRHCFMGVCSGKPGMVFSISRGIYSCIHGVAIEERQSVMNSPTATMNNTHSNILRLLRTAKNMANLSGVNGSPQSALDFIRRESSVYDISEHRRSFTHSDCKSYNNPPCEENLFSDYISEVERTFGNLQLKDSNVYQDHYHHHHRPHSIGSASSIDGLYDCDNPPFTTQSRSISKKPLDIGLPSSKHSQLSDLYGKFSFKSDRYSGHDDLIRSDVSDISTHTVTYGNIEGNAAKRRKQQYKDSLKKRPASAKSRREFDEIELAYRRRPPRSPDHKRYFRDKEGLRDFYLDQFRTKENSPHWEHVDLTDIYKERSDDFKRDSVSGGGPCTNRSHIKHGTGDKHGVVSGVPAPWEKNLTNVEWEDRSGGNFCRSCPSKLHNYSTTVTGQNSGRQACIRCEACKKAGNLYDISEDNSLQELDQPAAPVAVTSNASTTKYPQSPTNSKAQKKNRNKLRRQHSYDTFVDLQKEEAALAPRSVSLKDKGRFMDGSPYAHMFEMSAGESTFANNKSSVPTAGHHHHNNPGGGYMLSKSLYPDRVTQNPFIPTFGDDQCLLHGSKSYFFRQPTVAGASKARPDFRALVTNKPVVSALHGAVPARFQKDICIGNQSNPCVPNNKNPRAFNGSSNGHVYEKLSSIESDV
Show/Hide
|
||||
Organism |
Homo sapiens, Human
|
||||
Protein Classification |
Ion channel
>
Ligand-gated ion channel
>
Ionotropic glutamate receptor
>
NMDA receptor
|
||||
Function |
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).
Show/Hide
|
||||
Uniprot ID |
Show/Hide
|
||||
Ensembl ID | |||||
HGNC ID | |||||
Subcellular Location |
Cell membrane
Postsynaptic cell membrane
Late endosome
Lysosome
Cytoplasm
Cytoskeleton
|
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity |
|
---|
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Cell Line ID: CL000101 , L-M(TK-)
Cell Line ID: CL000041 , LTK-
Cell Line ID: CL000309 , NCTC clone 929
Biochemical Assays
Clinical Information about the Protein
Target 1 ( Glutamate receptor ionotropic NMDA 2B (NMDAR2B) )
Target Type | Successful Target | ||||
---|---|---|---|---|---|
Disease | 9 Target-related Diseases | 9 | |||
1 | Alpha-1 antitrypsin deficiency [ICD-11: 5C5A] | ||||
2 | Major depressive disorder [ICD-11: 6A70.3] | ||||
3 | Multiple sclerosis [ICD-11: 8A40] | ||||
4 | Peripheral neuropathy [ICD-11: 8C0Z] | ||||
5 | Neurological disorder [ICD-11: 6B60] | ||||
6 | Parkinson disease [ICD-11: 8A00.0] | ||||
7 | Cerebrovascular ischaemia [ICD-11: 8B1Z] | ||||
8 | Alzheimer disease [ICD-11: 8A20] | ||||
9 | Cancer related pain [ICD-11: MG30] | ||||
Approved Drug(s) | 1 Approved Drug | 1 | |||
1 | Alpha 1-PI | Approved | |||
Clinical Trial Drug(s) | 5 Clinical Trial Drugs | 5 | |||
1 | CERC-301 | Phase 2 | |||
2 | ELIPRODIL | Phase 2 | |||
3 | RGH-896 | Phase 2 | |||
4 | NBQX | Phase 1 | |||
5 | CP-101,606 | Phase 2 | |||
Discontinued Drug(s) | 6 Discontinued Drugs | 6 | |||
1 | Besonprodil | Discontinued in Phase 1 | |||
2 | DIZOCILPINE | Terminated | |||
3 | L-698532 | Terminated | |||
4 | L-698544 | Terminated | |||
5 | L-701324 | Terminated | |||
6 | RO-25-6981 | Terminated |
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID | Protein Name | Protein Organism | |
PT06444 | Glutamate receptor ionotropic, NMDA 2B | Mus musculus, Mouse |
---|