Details of the Target

General Information of Target

Target ID LDTP06370
Target Name Ephrin type-A receptor 7 (EPHA7)
Gene Name EPHA7
Gene ID 2045
Synonyms
EHK3; HEK11; Ephrin type-A receptor 7; EC 2.7.10.1; EPH homology kinase 3; EHK-3; EPH-like kinase 11; EK11; hEK11
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVFQTRYPSWIILCYIWLLRFAHTGEAQAAKEVLLLDSKAQQTELEWISSPPNGWEEISG
LDENYTPIRTYQVCQVMEPNQNNWLRTNWISKGNAQRIFVELKFTLRDCNSLPGVLGTCK
ETFNLYYYETDYDTGRNIRENLYVKIDTIAADESFTQGDLGERKMKLNTEVREIGPLSKK
GFYLAFQDVGACIALVSVKVYYKKCWSIIENLAIFPDTVTGSEFSSLVEVRGTCVSSAEE
EAENAPRMHCSAEGEWLVPIGKCICKAGYQQKGDTCEPCGRGFYKSSSQDLQCSRCPTHS
FSDKEGSSRCECEDGYYRAPSDPPYVACTRPPSAPQNLIFNINQTTVSLEWSPPADNGGR
NDVTYRILCKRCSWEQGECVPCGSNIGYMPQQTGLEDNYVTVMDLLAHANYTFEVEAVNG
VSDLSRSQRLFAAVSITTGQAAPSQVSGVMKERVLQRSVELSWQEPEHPNGVITEYEIKY
YEKDQRERTYSTVKTKSTSASINNLKPGTVYVFQIRAFTAAGYGNYSPRLDVATLEEATG
KMFEATAVSSEQNPVIIIAVVAVAGTIILVFMVFGFIIGRRHCGYSKADQEGDEELYFHF
KFPGTKTYIDPETYEDPNRAVHQFAKELDASCIKIERVIGAGEFGEVCSGRLKLPGKRDV
AVAIKTLKVGYTEKQRRDFLCEASIMGQFDHPNVVHLEGVVTRGKPVMIVIEFMENGALD
AFLRKHDGQFTVIQLVGMLRGIAAGMRYLADMGYVHRDLAARNILVNSNLVCKVSDFGLS
RVIEDDPEAVYTTTGGKIPVRWTAPEAIQYRKFTSASDVWSYGIVMWEVMSYGERPYWDM
SNQDVIKAIEEGYRLPAPMDCPAGLHQLMLDCWQKERAERPKFEQIVGILDKMIRNPNSL
KTPLGTCSRPISPLLDQNTPDFTTFCSVGEWLQAIKMERYKDNFTAAGYNSLESVARMTI
EDVMSLGITLVGHQKKIMSSIQTMRAQMLHLHGTGIQV
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, Ephrin receptor subfamily
Subcellular location
Cell membrane
Function
Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Among GPI-anchored ephrin-A ligands, EFNA5 is a cognate/functional ligand for EPHA7 and their interaction regulates brain development modulating cell-cell adhesion and repulsion. Has a repellent activity on axons and is for instance involved in the guidance of corticothalamic axons and in the proper topographic mapping of retinal axons to the colliculus. May also regulate brain development through a caspase(CASP3)-dependent proapoptotic activity. Forward signaling may result in activation of components of the ERK signaling pathway including MAP2K1, MAP2K2, MAPK1 and MAPK3 which are phosphorylated upon activation of EPHA7.
TTD ID
T57006
Uniprot ID
Q15375
DrugMap ID
TTAHTVG
Ensemble ID
ENST00000369297.1
HGNC ID
HGNC:3390
ChEMBL ID
CHEMBL4602

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 Insertion: p.E627GfsTer8 .
AU565 SNV: p.R366T .
CCLP1 SNV: p.R529G DBIA    Probe Info 
CFPAC1 SNV: p.Q675K .
EFO27 SNV: p.A213V .
HS936T SNV: p.D362N; p.G579R .
IGR1 SNV: p.K203Q .
KASUMI1 SNV: p.M893R .
KPL1 SNV: p.V418L .
MCF7 SNV: p.V418L .
MEWO SNV: p.E162K; p.S462F; p.G905E .
MOLM13 SNV: p.C250Y .
NCIH1793 SNV: p.W55C .
NCIH2172 SNV: p.I339N .
P31FUJ Substitution: p.G656V .
SNU1 SNV: p.K976E .
SNU5 SNV: p.A663V .
SSP25 SNV: p.G394V .
TE10 SNV: p.E56Ter .
TYKNU SNV: p.M893R .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
OPA-S-S-alkyne
 Probe Info  		K272(2.33)  LDD3494  [1]
DBIA
 Probe Info  		C296(1.79)  LDD3406  [2]
ATP probe
 Probe Info  		N.A.  LDD0199  [3]
IA-alkyne
 Probe Info  		C772(0.00); C648(0.00); C583(0.00); C681(0.00)  LDD0165  [4]
IPM
 Probe Info  		C772(0.00); C632(0.00)  LDD2156  [5]
PAL-AfBPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C170
 Probe Info  		16.00  LDD1850  [6]
C197
 Probe Info  		6.11  LDD1873  [6]
C208
 Probe Info  		6.54  LDD1883  [6]
C237
 Probe Info  		8.63  LDD1910  [6]
C310
 Probe Info  		30.27  LDD1977  [6]
C348
 Probe Info  		20.11  LDD2009  [6]
C349
 Probe Info  		13.55  LDD2010  [6]
C350
 Probe Info  		36.25  LDD2011  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A-549 C296(1.90); C293(1.40)  LDD2260  [2]
 LDCM0023  KB03 A-549 C296(2.57)  LDD2677  [2]
 LDCM0024  KB05 RKN C296(1.79)  LDD3406  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Macrophage colony-stimulating factor 1 receptor (CSF1R) Tyr protein kinase family P07333
Ephrin type-A receptor 2 (EPHA2) Tyr protein kinase family P29317
Ephrin type-A receptor 3 (EPHA3) Tyr protein kinase family P29320
Ephrin type-B receptor 2 (EPHB2) Tyr protein kinase family P29323
Ephrin type-B receptor 4 (EPHB4) Tyr protein kinase family P54760
NT-3 growth factor receptor (NTRK3) Tyr protein kinase family Q16288

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid19788238c66 Small molecular drug D05FXD
Pmid21561767c8h Small molecular drug D02BXJ
Pmid23489211c20 Small molecular drug D0X8BU
5-[(2-methyl-5-{[3-(Trifluoromethyl)Phenyl]Carbamoyl}Phenyl)Amino]Pyridine-3-carboxamide . DB07970

References

1 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
4 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
5 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
6 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587