Details of the Target

General Information of Target

Target ID LDTP05720
Target Name Glutamate receptor ionotropic, kainate 2 (GRIK2)
Gene Name GRIK2
Gene ID 2898
Synonyms
GLUR6; Glutamate receptor ionotropic, kainate 2; GluK2; Excitatory amino acid receptor 4; EAA4; Glutamate receptor 6; GluR-6; GluR6
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKIIFPILSNPVFRRTVKLLLCLLWIGYSQGTTHVLRFGGIFEYVESGPMGAEELAFRFA
VNTINRNRTLLPNTTLTYDTQKINLYDSFEASKKACDQLSLGVAAIFGPSHSSSANAVQS
ICNALGVPHIQTRWKHQVSDNKDSFYVSLYPDFSSLSRAILDLVQFFKWKTVTVVYDDST
GLIRLQELIKAPSRYNLRLKIRQLPADTKDAKPLLKEMKRGKEFHVIFDCSHEMAAGILK
QALAMGMMTEYYHYIFTTLDLFALDVEPYRYSGVNMTGFRILNTENTQVSSIIEKWSMER
LQAPPKPDSGLLDGFMTTDAALMYDAVHVVSVAVQQFPQMTVSSLQCNRHKPWRFGTRFM
SLIKEAHWEGLTGRITFNKTNGLRTDFDLDVISLKEEGLEKIGTWDPASGLNMTESQKGK
PANITDSLSNRSLIVTTILEEPYVLFKKSDKPLYGNDRFEGYCIDLLRELSTILGFTYEI
RLVEDGKYGAQDDANGQWNGMVRELIDHKADLAVAPLAITYVREKVIDFSKPFMTLGISI
LYRKPNGTNPGVFSFLNPLSPDIWMYILLAYLGVSCVLFVIARFSPYEWYNPHPCNPDSD
VVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLT
VERMESPIDSADDLAKQTKIEYGAVEDGATMTFFKKSKISTYDKMWAFMSSRRQSVLVKS
NEEGIQRVLTSDYAFLMESTTIEFVTQRNCNLTQIGGLIDSKGYGVGTPMGSPYRDKITI
AILQLQEEGKLHMMKEKWWRGNGCPEEESKEASALGVQNIGGIFIVLAAGLVLSVFVAVG
EFLYKSKKNAQLEKRSFCSAMVEELRMSLKCQRRLKHKPQAPVIVKTEEVINMHTFNDRR
LPGKETMA
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Glutamate-gated ion channel (TC 1.A.10.1) family, GRIK2 subfamily
Subcellular location
Cell membrane
Function
Ionotropic glutamate receptor. 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. Modulates cell surface expression of NETO2.; Independent of its ionotropic glutamate receptor activity, acts as a thermoreceptor conferring sensitivity to cold temperatures. Functions in dorsal root ganglion neurons.
TTD ID
T58178
Uniprot ID
Q13002
DrugMap ID
TT0K5RG
Ensemble ID
ENST00000369134.9
HGNC ID
HGNC:4580
ChEMBL ID
CHEMBL3683

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.T740I .
HCT116 SNV: p.V35A .
HCT15 SNV: p.I699T; p.T906I .
HELA SNV: p.A490V .
HT SNV: p.K544R .
HT115 SNV: p.S649Y .
IGR1 SNV: p.S650L .
JURKAT SNV: p.K379N .
MCC13 Substitution: p.P109F .
MEWO SNV: p.G500R; p.E796K .
NCIH716 SNV: p.R354C .
OVK18 SNV: p.T357P .
SW1271 Deletion: p.P667LfsTer8
SNV: p.Q339K;p.R431P		 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
ONAyne
 Probe Info  		K212(4.42)  LDD0275  [1]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270