Id: acc0489
Group: 1sens
Protein: FAK
Gene Symbol: PTK2
Protein Id: Q05397
Protein Name: FAK1_HUMAN
PTM: phosphorylation
Site: Tyr397
Site Sequence: AVSVSETDDYAEIIDEEDTYT
Disease Category: Cancer
Disease: Hepatocellular Carcinoma
Disease Subtype:
Disease Cellline: Bel-7402
Disease Info:
Drug: cabozantinib
Drug Info: "Cabozantinib is a multi-targeted tyrosine kinase inhibitor that acts on MET, VEGFR1/2/3, RET, AXL, and other kinases, approved for the treatment of progressive metastatic medullary thyroid cancer, advanced renal cell carcinoma after prior anti-angiogenic therapy, and hepatocellular carcinoma following sorafenib failure. "
Effect: inhibit
Effect Info: "CT-707 significantly reduces cabozantinib-induced FAK phosphorylation, thereby reducing cabozantinib-induced tumor resistance."
Note:
Score: 5.0
Pubmed(PMID): 27638856
Sentence Index:
Sentence:

Sequence & Structure:

MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFIIRPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRERIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDHPHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESKRFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFTSASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWAYDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGYPSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQEIAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLSRGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNEGVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLALRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQMLTAAHALAVDAKNLLDVIDQARLKMLGQTRPH

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 3 Recruiting ovarian cancer ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Terminated malignant pleural mesothelioma ClinicalTrials
ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Active, not recruiting multiple myeloma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting pancreatic carcinoma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting thyroid carcinoma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Active, not recruiting ovarian serous adenocarcinoma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting pancreatic adenocarcinoma ClinicalTrials
PTK2 GSK-2256098 Focal adhesion kinase 1 inhibitor 2 Completed pancreatic adenocarcinoma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Active, not recruiting Uveal Melanoma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting pancreatic ductal adenocarcinoma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Not yet recruiting colorectal cancer ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Active, not recruiting ovarian cancer ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting ovarian cancer ClinicalTrials
PTK2 IFEBEMTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting ovarian cancer ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Completed lung cancer ClinicalTrials
PTK2 GSK-2256098 Focal adhesion kinase 1 inhibitor 2 Recruiting meningioma ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 2 Recruiting female reproductive system neoplasm ClinicalTrials
PTK2 GSK-2256098 Focal adhesion kinase 1 inhibitor 2 Recruiting intracranial meningioma ClinicalTrials
PTK2 VS-4718 Focal adhesion kinase 1 inhibitor 1 Withdrawn B-cell acute lymphoblastic leukemia ClinicalTrials
PTK2 VS-4718 Focal adhesion kinase 1 inhibitor 1 Withdrawn acute myeloid leukemia ClinicalTrials
PTK2 DEFACTINIB Focal adhesion kinase 1 inhibitor 1 Active, not recruiting endometrioid carcinoma ClinicalTrials
PTK2 IFEBEMTINIB Focal adhesion kinase 1 inhibitor 1 Not yet recruiting neoplasm ClinicalTrials
PTK2 IFEBEMTINIB Focal adhesion kinase 1 inhibitor 1 Recruiting neoplasm ClinicalTrials
ClinicalTrials
PTK2 CEP-37440 Focal adhesion kinase 1 inhibitor 1 Completed neoplasm 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
PTK2-Tyr397
Cancer Intensity
BRCA
COAD 0.587
HGSC -1.155
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.567

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 397 D Skin cancer Phosphorylation 23799510
Y 397 D Colorectal cancer Phosphorylation 12871985 ;  12871985
Y 397 D Lung cancer/carcinoma Phosphorylation 23799510
Y 397 D Lung cancer Phosphorylation 21876001
Y 397 D Hepatocellular carcinoma Phosphorylation 36209205
Y 397 P Gastric cancer Phosphorylation 23109808
Y 397 U Papillary thyroid carcinoma Phosphorylation 37443754
Y 397 U Melanoma Phosphorylation 24098450
Y 397 U Lung squamous cell carcinoma Phosphorylation 23906871
Y 397 U Breast cancer Phosphorylation 37846507
Y 397 U Oral squamous cell carcinoma Phosphorylation 22766511
Y 397 U Ovarian cancer/carcinoma Phosphorylation 24062525
Y 397 U Ovarian epithelial carcinoma Phosphorylation 24655477
Y 397 U Non-small cell lung cancer Phosphorylation 36209201
Y 397 U Glioblastoma Phosphorylation 23243059
Y 397 U Ewing sarcoma Phosphorylation 31811703
Y 397 U Ovarian epithelial carcinoma Phosphorylation 24655477
Y 397 U Ovarian cancer/carcinoma Phosphorylation 24655477
Y 397 U Squamous cell carcinoma Phosphorylation 14603053 ;  14603053 ;  14603053
Y 397 U Osteosarcoma Phosphorylation 37013056
Y 397 U Diffuse gastric cancer Phosphorylation 35471457
Y 397 U Clear cell renal cell carcinoma Phosphorylation 35257717
Y 397 U Cancer Phosphorylation 14603053 ;  14603053
Y 397 U Non-small cell lung cancer Phosphorylation 35131384
Y 397 U Hepatocellular carcinoma/hepatocarcinoma/hepatoma Phosphorylation 23525457 ;  20180147
Y 397 U Esophageal squamous cell carcinoma Phosphorylation 33532186
Y 397 U Ovarian cancer Phosphorylation 37221403 ;  35201437
Y 397 U Pancreatic ductal adenocarcinoma Phosphorylation 35982848 ;  36228156

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: