Details of the Target

General Information of Target

Target ID LDTP03476
Target Name Ephrin type-A receptor 8 (EPHA8)
Gene Name EPHA8
Gene ID 2046
Synonyms
EEK; HEK3; KIAA1459; Ephrin type-A receptor 8; EC 2.7.10.1; EPH- and ELK-related kinase; EPH-like kinase 3; EK3; hEK3; Tyrosine-protein kinase receptor EEK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAPARGRLPPALWVVTAAAAAATCVSAARGEVNLLDTSTIHGDWGWLTYPAHGWDSINEV
DESFQPIHTYQVCNVMSPNQNNWLRTSWVPRDGARRVYAEIKFTLRDCNSMPGVLGTCKE
TFNLYYLESDRDLGASTQESQFLKIDTIAADESFTGADLGVRRLKLNTEVRSVGPLSKRG
FYLAFQDIGACLAILSLRIYYKKCPAMVRNLAAFSEAVTGADSSSLVEVRGQCVRHSEER
DTPKMYCSAEGEWLVPIGKCVCSAGYEERRDACVACELGFYKSAPGDQLCARCPPHSHSA
APAAQACHCDLSYYRAALDPPSSACTRPPSAPVNLISSVNGTSVTLEWAPPLDPGGRSDI
TYNAVCRRCPWALSRCEACGSGTRFVPQQTSLVQASLLVANLLAHMNYSFWIEAVNGVSD
LSPEPRRAAVVNITTNQAAPSQVVVIRQERAGQTSVSLLWQEPEQPNGIILEYEIKYYEK
DKEMQSYSTLKAVTTRATVSGLKPGTRYVFQVRARTSAGCGRFSQAMEVETGKPRPRYDT
RTIVWICLTLITGLVVLLLLLICKKRHCGYSKAFQDSDEEKMHYQNGQAPPPVFLPLHHP
PGKLPEPQFYAEPHTYEEPGRAGRSFTREIEASRIHIEKIIGSGDSGEVCYGRLRVPGQR
DVPVAIKALKAGYTERQRRDFLSEASIMGQFDHPNIIRLEGVVTRGRLAMIVTEYMENGS
LDTFLRTHDGQFTIMQLVGMLRGVGAGMRYLSDLGYVHRDLAARNVLVDSNLVCKVSDFG
LSRVLEDDPDAAYTTTGGKIPIRWTAPEAIAFRTFSSASDVWSFGVVMWEVLAYGERPYW
NMTNRDVISSVEEGYRLPAPMGCPHALHQLMLDCWHKDRAQRPRFSQIVSVLDALIRSPE
SLRATATVSRCPPPAFVRSCFDLRGGSGGGGGLTVGDWLDSIRMGRYRDHFAAGGYSSLG
MVLRMNAQDVRALGITLMGHQKKILGSIQTMRAQLTSTQGPRRHL
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. The GPI-anchored ephrin-A EFNA2, EFNA3, and EFNA5 are able to activate EPHA8 through phosphorylation. With EFNA5 may regulate integrin-mediated cell adhesion and migration on fibronectin substrate but also neurite outgrowth. During development of the nervous system also plays a role in axon guidance. Downstream effectors of the EPHA8 signaling pathway include FYN which promotes cell adhesion upon activation by EPHA8 and the MAP kinases in the stimulation of neurite outgrowth.
TTD ID
T58266
Uniprot ID
P29322
DrugMap ID
TTHZ2LW
Ensemble ID
ENST00000166244.8
HGNC ID
HGNC:3391
ChEMBL ID
CHEMBL4134

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO320 SNV: p.W938Ter .
COLO792 SNV: p.V72A .
COLO800 Substitution: p.E629K .
HCC1395 SNV: p.N123K .
HCT15 SNV: p.E714A .
HT115 SNV: p.M861R .
HT29 SNV: p.W545Ter .
JHH1 SNV: p.R91L .
JVM3 SNV: p.A190S .
KASUMI1 SNV: p.N844S .
KMRC1 SNV: p.Y200C .
MELJUSO SNV: p.W545Ter .
NCIH1155 SNV: p.A894T .
OVCAR5 SNV: p.S225Ter .
RAMOS SNV: p.R764L .
SNU869 SNV: p.A622V .
SW480 SNV: p.G936V .
TE10 SNV: p.H567Y .
TOV21G SNV: p.L490I .
WM793 SNV: p.S77I .

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
BTD
 Probe Info  		C520(1.41)  LDD2090  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C520(1.41)  LDD2090  [1]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C520(0.72)  LDD2153  [1]

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761