Id: acc0582
Group: 1sens
Protein: EphA2
Gene Symbol: EPHA2
Protein Id: P29317
Protein Name: EPHA2_HUMAN
PTM: phosphorylation
Site: Tyr558
Site Sequence: LVLAGVGFFIHRRRKNQRARQ
Disease Category: Cancer
Disease: Ovarian Cancer
Disease Subtype: high-grade serous ovarian cancer
Disease Cellline: OVCAR4
Disease Info:
Drug: platinum
Drug Info: "Cisplatin: A platinum-containing chemotherapeutic agent used in the treatment of various cancers, including testicular, ovarian, and lung cancers, by forming DNA adducts that inhibit cancer cell replication. Carboplatin: A second-generation platinum-based antineoplastic drug with reduced nephrotoxicity compared to cisplatin, commonly employed in ovarian cancer and other malignancies. Oxaliplatin: A third-generation platinum compound effective against colorectal cancer, characterized by its distinct mechanism of action and reduced cross-resistance with other platinum drugs. "
Effect: promote
Effect Info: RSK inhibitors can enhance the therapeutic effect of cisplatin by inhibiting the phosphorylation of EphA2 at S897 and restoring the phosphorylation at Y588.
Note:
Score: 5.0
Pubmed(PMID): 32115889
Sentence Index:
Sentence:

Sequence & Structure:

MELQAARACFALLWGCALAAAAAAQGKEVVLLDFAAAGGELGWLTHPYGKGWDLMQNIMNDMPIYMYSVCNVMSGDQDNWLRTNWVYRGEAERIFIELKFTVRDCNSFPGGASSCKETFNLYYAESDLDYGTNFQKRLFTKIDTIAPDEITVSSDFEARHVKLNVEERSVGPLTRKGFYLAFQDIGACVALLSVRVYYKKCPELLQGLAHFPETIAGSDAPSLATVAGTCVDHAVVPPGGEEPRMHCAVDGEWLVPIGQCLCQAGYEKVEDACQACSPGFFKFEASESPCLECPEHTLPSPEGATSCECEEGFFRAPQDPASMPCTRPPSAPHYLTAVGMGAKVELRWTPPQDSGGREDIVYSVTCEQCWPESGECGPCEASVRYSEPPHGLTRTSVTVSDLEPHMNYTFTVEARNGVSGLVTSRSFRTASVSINQTEPPKVRLEGRSTTSLSVSWSIPPPQQSRVWKYEVTYRKKGDSNSYNVRRTEGFSVTLDDLAPDTTYLVQVQALTQEGQGAGSKVHEFQTLSPEGSGNLAVIGGVAVGVVLLLVLAGVGFFIHRRRKNQRARQSPEDVYFSKSEQLKPLKTYVDPHTYEDPNQAVLKFTTEIHPSCVTRQKVIGAGEFGEVYKGMLKTSSGKKEVPVAIKTLKAGYTEKQRVDFLGEAGIMGQFSHHNIIRLEGVISKYKPMMIITEYMENGALDKFLREKDGEFSVLQLVGMLRGIAAGMKYLANMNYVHRDLAARNILVNSNLVCKVSDFGLSRVLEDDPEATYTTSGGKIPIRWTAPEAISYRKFTSASDVWSFGIVMWEVMTYGERPYWELSNHEVMKAINDGFRLPTPMDCPSAIYQLMMQCWQQERARRPKFADIVSILDKLIRAPDSLKTLADFDPRVSIRLPSTSGSEGVPFRTVSEWLESIKMQQYTEHFMAAGYTAIEKVVQMTNDDIKRIGVRLPGHQKRIAYSLLGLKDQVNTVGIPI

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 Unknown status acute lymphoblastic leukemia ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 - acute lymphoblastic leukemia DailyMed
DailyMed
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 - chronic myelogenous leukemia DailyMed
DailyMed
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 Completed chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 Recruiting chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 Unknown status chronic myelogenous leukemia ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 - neoplasm ATC
EPHA2 REGORAFENIB Ephrin type-A receptor 2 4 - neoplasm ATC
EPHA2 VANDETANIB Ephrin receptor inhibitor 4 - neoplasm ATC
EPHA2 VANDETANIB Ephrin receptor inhibitor 4 - thyroid carcinoma DailyMed
EPHA2 VANDETANIB Ephrin receptor inhibitor 4 - thyroid neoplasm EMA
EPHA2 REGORAFENIB Ephrin type-A receptor 2 4 - colorectal neoplasm EMA
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 - lymphoid leukemia EMA
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 4 - Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive EMA
EPHA2 VANDETANIB Ephrin receptor inhibitor 4 Active, not recruiting thyroid cancer ClinicalTrials
EPHA2 VANDETANIB Ephrin receptor inhibitor 4 - medullary thyroid gland carcinoma DailyMed
EPHA2 REGORAFENIB Ephrin type-A receptor 2 3 Recruiting hepatocellular carcinoma ClinicalTrials
EPHA2 REGORAFENIB Ephrin type-A receptor 2 3 Terminated hepatocellular carcinoma ClinicalTrials
EPHA2 REGORAFENIB Ephrin type-A receptor 2 3 Completed hepatocellular carcinoma ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 3 Completed acute lymphoblastic leukemia ClinicalTrials
ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 3 Completed acute myeloid leukemia ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 3 Active, not recruiting acute lymphoblastic leukemia ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 3 Not yet recruiting acute lymphoblastic leukemia ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 3 Terminated chronic myelogenous leukemia ClinicalTrials
EPHA2 DASATINIB Ephrin type-A receptor 2 inhibitor 3 Active, not recruiting chronic myelogenous leukemia ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No intensity data of this site,
show all other sites!

EPHA2-Ser516
Cancer Intensity
BRCA
COAD
HGSC 1.828
ccRCC 0.406
GBM
HNSC
LUAD -0.525
LUSC -0.679
non_ccRCC -0.852
PDAC -0.177
UCEC
EPHA2-Ser838
Cancer Intensity
BRCA
COAD
HGSC 1.368
ccRCC -0.754
GBM -1.001
HNSC
LUAD
LUSC 0.769
non_ccRCC -1.021
PDAC 0.919
UCEC -0.28
EPHA2-Ser843
Cancer Intensity
BRCA
COAD
HGSC 1.069
ccRCC -0.155
GBM -0.913
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
EPHA2-Ser845
Cancer Intensity
BRCA
COAD -1.151
HGSC
ccRCC 0.66
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.491
EPHA2-Ser847
Cancer Intensity
BRCA
COAD -0.72
HGSC
ccRCC 0.912
GBM -0.309
HNSC
LUAD
LUSC -1.491
non_ccRCC 1.471
PDAC -0.212
UCEC 0.349
EPHA2-Thr844
Cancer Intensity
BRCA
COAD
HGSC 0.707
ccRCC -0.707
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
EPHA2-Tyr521
Cancer Intensity
BRCA
COAD -0.304
HGSC
ccRCC
GBM -0.476
HNSC
LUAD 1.684
LUSC -0.255
non_ccRCC -1.21
PDAC 0.561
UCEC
EPHA2-Tyr540
Cancer Intensity
BRCA
COAD
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC -0.707
PDAC
UCEC
EPHA2-Tyr718
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 772 D Ewing sarcoma Phosphorylation 36394520
S 897 D Ewing sarcoma Phosphorylation 36394520
S 897 P Cancer Phosphorylation 35668076
S 897 U Breast cancer Phosphorylation 23772378
S 897 U Cervical cancer/carcinoma Phosphorylation 23772378
S 897 U Lung cancer Phosphorylation 26158630
Y 772 U Nasopharyngeal carcinoma Phosphorylation 32848131
- - U Gastric cancer Phosphorylation 15649254
S 897 U Glioblastoma Phosphorylation 19573808 ;  35124461
S 897 U Thyroid cancer Phosphorylation 32762307
S 897 U Hepatocellular carcinoma Phosphorylation 34484860

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: