Id: acc0775
Group: 2sens
Protein: FAK
Gene Symbol: PTK2
Protein Id: Q05397
Protein Name: FAK1_HUMAN
PTM: phosphorylation
Site: Tyr576
Site Sequence: LSRYMEDSTYYKASKGKLPIK
Disease Category: Cancer
Disease: Prostate Cancer
Disease Subtype:
Disease Cellline: LNCaP C4-2B
Disease Info:
Drug: apigenin
Drug Info: "Apigenin is a naturally occurring flavonoid compound with demonstrated potential as an antifungal agent in the preparation of drugs against human fungal infections, and it is also being researched in drug delivery systems such as solid lipid nanoparticles (APG-SLNP) to enhance stability and bioavailability. "
Effect: modulate
Effect Info: "Apigenin inhibits prostate carcinogenesis by suppressing the phosphorylation of Smad2/3, Src, FAK, and Akt."
Note:
Score: 4.0
Pubmed(PMID): 23359392
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-Tyr576
Cancer Intensity
BRCA
COAD 0.473
HGSC 1.142
ccRCC
GBM -0.517
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC -1.098

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 576 D Hepatocellular carcinoma Phosphorylation 36209205
Y 576 D X-linked agammaglobulinemia Phosphorylation 22366891
Y 576 U High-grade serous ovarian cancer Phosphorylation 35467979

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
Q05397 PTK2 P Tyr576 YMEDSTY(ph)YK A431 Imatinib 8.2423 -
Q05397 PTK2 P Ser574;Thr575;Tyr576;Tyr577 YMEDS(ph)T(ph)Y(ph)Y(ph)K PC-9 AZD4547 1.5229 -
Q05397 PTK2 P Tyr576 YMEDSTY(ph)YK PC-9 Gefitinib 4.9948 -
Q05397 PTK2 P Tyr576 YMEDSTY(ph)YK PC-9 GeftinibAZD4547-1to80 6.6249 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: