Molecular Target
Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Cellline Data Matrix
Gene Expression
Gene Copy Number Variation
RNA Interference
Mutations

GRIN3A (Q8TCU5) - Overview - Molecular Target Synopsis



Protein


GRIN3A, Glutamate receptor ionotropic, NMDA 3A
UniProt Q8TCU5

Also Known as NMD3A_HUMAN, GRIN3A, KIAA1973

NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May play a role in the development of dendritic spines. May play a role in PPP2CB-NMDAR mediated signaling mechanism. Forms heteromeric channel of a zeta subunit (GRIN1), a epsilon subunit (GRIN2A, GRIN2B, GRIN2C or GRIN2D) and a third subunit (GRIN3A or GRIN3B). Does not form functional homomeric channels. Found in a complex with GRIN1, GRIN2A or GRIN2B and PPP2CB. Probably interacts with PPP2CB. No complex with PPP2CB is detected when NMDARs are stimulated by NMDA.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1115ENSG00000198785ENST00000361820ENSP00000355155Q8TCU5-1

Sequences


ENSG00000198785, ENST00000361820, ENSP00000355155, Q8TCU5

MRRLSLWWLL SRVCLLLPPP CALVLAGVPS SSSHPQPCQI LKRIGHAVRV 
GAVHLQPWTT APRAASRAPD DSRAGAQRDE PEPGTRRSPA PSPGARWLGS
TLHGRGPPGS RKPGEGARAE ALWPRDALLF AVDNLNRVEG LLPYNLSLEV
VMAIEAGLGD LPLLPFSSPS SPWSSDPFSF LQSVCHTVVV QGVSALLAFP
QSQGEMMELD LVSLVLHIPV ISIVRHEFPR ESQNPLHLQL SLENSLSSDA
DVTVSILTMN NWYNFSLLLC QEDWNITDFL LLTQNNSKFH LGSIINITAN
LPSTQDLLSF LQIQLESIKN STPTVVMFGC DMESIRRIFE ITTQFGVMPP
ELRWVLGDSQ NVEELRTEGL PLGLIAHGKT TQSVFEHYVQ DAMELVARAV
ATATMIQPEL ALIPSTMNCM EVETTNLTSG QYLSRFLANT TFRGLSGSIR
VKGSTIVSSE NNFFIWNLQH DPMGKPMWTR LGSWQGGKIV MDYGIWPEQA
QRHKTHFQHP SKLHLRVVTL IEHPFVFTRE VDDEGLCPAG QLCLDPMTND
SSTLDSLFSS LHSSNDTVPI KFKKCCYGYC IDLLEKIAED MNFDFDLYIV
GDGKYGAWKN GHWTGLVGDL LRGTAHMAVT SFSINTARSQ VIDFTSPFFS
TSLGILVRTR DTAAPIGAFM WPLHWTMWLG IFVALHITAV FLTLYEWKSP
FGLTPKGRNR SKVFSFSSAL NICYALLFGR TVAIKPPKCW TGRFLMNLWA
IFCMFCLSTY TANLAAVMVG EKIYEELSGI HDPKLHHPSQ GFRFGTVRES
SAEDYVRQSF PEMHEYMRRY NVPATPDGVE YLKNDPEKLD AFIMDKALLD
YEVSIDADCK LLTVGKPFAI EGYGIGLPPN SPLTANISEL ISQYKSHGFM
DMLHDKWYRV VPCGKRSFAV TETLQMGIKH FSGLFVLLCI GFGLSILTTI
GEHIVYRLLL PRIKNKSKLQ YWLHTSQRLH RAINTSFIEE KQQHFKTKRV
EKRSNVGPRQ LTVWNTSNLS HDNRRKYIFS DEEGQNQLGI RIHQDIPLPP
RRRELPALRT TNGKADSLNV SRNSVMQELS ELEKQIQVIR QELQLAVSRK
TELEEYQRTS RTCES

Sub-cellular localization


UniProt: GRIN3A is active in the following subcellular-locations: Cell junction, Cell membrane, postsynaptic cell membrane, postsynaptic density, synapse.
GO terms: GRIN3A is active in the following subcellular-locations: cell junction, dendrite, integral component of membrane, membrane, N-methyl-D-aspartate selective glutamate receptor complex, neuron projection, neuronal cell body, postsynaptic density, postsynaptic membrane, synapse.



UniProt
GO terms

Mutations in Cancer


In COSMIC - Cell Lines Project there are 106 unique mutations of GRIN3A: p.? (3), p.R1009C (2), p.Y493F (2), p.E205K (1), p.L1082P (1), p.M473I (1), p.G114R (1), p.P879T (1), p.A397T (1), p.V457I (1), p.G99G (1), p.I218V (1), p.I295S (1), p.G601E (1), p.I256I (1), p.I666T (1), p.D471G (1), p.M207V (1), p.S650F (1), p.S650S (1), p.W97C (1), p.C330C (1), p.Y873Y (1), p.K833N (1), p.L673H (1), p.P700L (1), p.T1101M (1), p.P108L (1), p.R398G (1), p.F199L (1), p.G159A (1), p.P878T (1), p.S789F (1), p.G94G (1), p.P302S (1), p.G1034R (1), p.G159G (1), p.Y695* (1), p.G106V (1), p.S564N (1), p.G140G (1), p.E155E (1), p.T380A (1), p.L315I (1), p.C913S (1), p.N275N (1), p.I154I (1), p.A824T (1), p.L269L (1), p.G680G (1), p.A131A (1), p.S245L (1), p.E386Q (1), p.W749R (1), p.T187T (1), p.T761K (1), p.A725A (1), p.V767I (1), p.K772N (1), p.G779G (1), p.R708Q (1), p.E696K (1), p.G578E (1), p.D596N (1), p.L616L (1), p.P665P (1), p.P783H (1), p.K784N (1), p.E1033K (1), p.V1013A (1), p.R1072Q (1), p.E1104K (1), p.E364K (1), p.S1004T (1), p.K966N (1), p.D845G (1), p.D858N (1), p.F899F (1), p.T921M (1), p.V531V (1), p.V518I (1), p.L257L (1), p.E227K (1), p.T258T (1), p.K288N (1), p.T298T (1), p.R225H (1), p.G204D (1), p.S179S (1), p.R225C (1), p.Q201fs*6 (1), p.S202S (1), p.Q312Q (1), p.R337R (1), p.R443R (1), p.F442F (1), p.G453D (1), p.H509L (1), p.P510S (1), p.Q431P (1), p.V422V (1), p.R353C (1), p.T380T (1), p.E394K (1), p.N418Y (1), p.G157C (1)
In COSMIC there are 280 unique mutations of GRIN3A: p.S171L (6), p.E340K (4), p.E364K (3), p.? (3), p.L544L (3), p.M405I (2), p.F931L (2), p.R638R (2), p.L673H (2), p.N984N (2), p.A299T (2), p.S789F (2), p.F595F (2), p.L727L (2), p.L209L (2), p.R708* (2), p.W678* (2), p.R353C (2), p.I223I (2), p.Y873Y (2), p.M591I (2), p.T343A (2), p.R225C (2), p.R1041Q (2), p.P229L (2), p.G474E (2), p.L620L (2), p.M817I (2), p.H103Y (2), p.G578R (1), p.S415N (1), p.S232N (1), p.I1028I (1), p.M332I (1), p.V193M (1), p.F463I (1), p.A750G (1), p.K968K (1), p.Q284K (1), p.R1059R (1), p.A131D (1), p.G487E (1), p.R1009H (1), p.I954T (1), p.G654C (1), p.A689A (1), p.A689S (1), p.S309S (1), p.L726L (1), p.P93P (1), p.G535G (1), p.G540D (1), p.W466* (1), p.E696K (1), p.D804H (1), p.P1008P (1), p.W613* (1), p.L141>? (1), p.T304P (1), p.D160fs*47 (1), p.R366M (1), p.I456V (1), p.H781Y (1), p.N296N (1), p.T404T (1), p.K833R (1), p.D278N (1), p.P169H (1), p.L694M (1), p.S511G (1), p.D643H (1), p.E231E (1), p.P700L (1), p.E952K (1), p.E771K (1), p.P107P (1), p.L308F (1), p.W478* (1), p.V457I (1), p.A637V (1), p.Y598Y (1), p.E1078K (1), p.R962Q (1), p.Q314* (1), p.V617L (1), p.G204G (1), p.A195V (1), p.L515F (1), p.G779* (1), p.L216P (1), p.C419C (1), p.V629V (1), p.I870M (1), p.C859Y (1), p.N418T (1), p.Q233E (1), p.G865R (1), p.S446G (1), p.L883* (1), p.P672L (1), p.T884T (1), p.L727S (1), p.F691F (1), p.A637E (1), p.K512M (1), p.E889K (1), p.P1047S (1), p.R230W (1), p.W740C (1), p.S194L (1), p.V254A (1), p.R957S (1), p.C270W (1), p.S415R (1), p.P1008L (1), p.G373G (1), p.A637A (1), p.I687I (1), p.A762T (1), p.D160Y (1), p.L764M (1), p.W354L (1), p.G487G (1), p.M746I (1), p.V1000V (1), p.V254I (1), p.G106W (1), p.G603E (1), p.M259L (1), p.W274C (1), p.R708Q (1), p.R1059W (1), p.W478L (1), p.Y144C (1), p.D582N (1), p.A127V (1), p.T659N (1), p.I870T (1), p.S167F (1), p.H897H (1), p.L944M (1), p.K772K (1), p.K784E (1), p.D471Y (1), p.S888S (1), p.L308L (1), p.E871A (1), p.R1090C (1), p.N136D (1), p.V767F (1), p.R1059Q (1), p.R43H (1), p.L861R (1), p.E989E (1), p.I465I (1), p.Q305R (1), p.C185W (1), p.H612N (1), p.E852K (1), p.L947L (1), p.P349L (1), p.S454P (1), p.Q1037fs*32 (1), p.S194S (1), p.C330C (1), p.N747T (1), p.N260S (1), p.S241S (1), p.T659A (1), p.E534K (1), p.L748I (1), p.D79N (1), p.D532Y (1), p.G114A (1), p.I335I (1), p.Q541K (1), p.S454T (1), p.V396A (1), p.A857V (1), p.E585K (1), p.G346A (1), p.S454F (1), p.D590D (1), p.V389I (1), p.D845N (1), p.G828R (1), p.P200P (1), p.P826R (1), p.S511R (1), p.D594V (1), p.W608* (1), p.P200S (1), p.A119E (1), p.D1045N (1), p.A885T (1), p.Q469Q (1), p.I983L (1), p.T659T (1), p.F279V (1), p.S359S (1), p.W907C (1), p.D840D (1), p.V911F (1), p.S454C (1), p.E364Q (1), p.N834K (1), p.I687N (1), p.S717Y (1), p.F279F (1), p.L135L (1), p.P879T (1), p.G373W (1), p.L692F (1), p.M417I (1), p.N261K (1), p.N300S (1), p.G874R (1), p.R638G (1), p.A733T (1), p.E460K (1), p.M768V (1), p.D545A (1), p.T283T (1), p.N264H (1), p.F464F (1), p.R137H (1), p.A52A (1), p.E205K (1), p.M477L (1), p.S881F (1), p.G615A (1), p.S1030T (1), p.L597L (1), p.V713V (1), p.S245* (1), p.G865W (1), p.V864V (1), p.G943R (1), p.G791* (1), p.R660R (1), p.I954M (1), p.V396V (1), p.S560I (1), p.R96C (1), p.S758F (1), p.S248Y (1), p.G742R (1), p.D545H (1), p.P705L (1), p.C537F (1), p.W173* (1), p.D850N (1), p.S245L (1), p.D249Y (1), p.R1025W (1), p.D835N (1), p.V490F (1), p.G494E (1), p.G603* (1), p.P472P (1), p.R916I (1), p.N834N (1), p.V252V (1), p.R337W (1), p.L554L (1), p.L216M (1), p.E120K (1), p.Q344* (1), p.W697* (1), p.E1102K (1), p.R978K (1), p.F310F (1), p.I318T (1), p.I449M (1), p.G487R (1), p.A607A (1), p.K1100R (1), p.P165L (1), p.S511S (1), p.G369V (1)
Please click the link to see mutations reported in Cancer Gene Census
Please click the link to see mutations reported in ICGC
(see details)

Gene Expression


In the NCI - NCI 60 Reference panel, the highest expressing cell lines are: ACHN, HS578T. (see details)

RNA Interference


GRIN3A was reported in the following RNAI studies:

AACR Journals - Results of primary druggable genome v2 (DG2) Achilles heel siRNA screen in KMS11 multiple myeloma cells, the highest RNAi cell lines are: KMS11. (see details)


Screening and Chemistry


GRIN3A has been screened with 458 compounds (705 bioactivities), 165 compounds have bioactivities that show binding affinity of <= 500nM (198 bioactivities). (see details)