Id: acc0302
Group: 1sens
Protein: FAK
Gene Symbol: PTK2
Protein Id: Q05397
Protein Name: FAK1_HUMAN
PTM: phosphorylation
Site: Tyr576
Site Sequence: LSRYMEDSTYYKASKGKLPIK
Disease Category: Cancer
Disease: Sarcoma
Disease Subtype: synovial sarcoma
Disease Cellline: CME-1
Disease Info:
Drug: dasatinib
Drug Info: "Dasatinib is a tyrosine kinase inhibitor that targets BCR-ABL and SRC family kinases, used in the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), particularly in patients resistant or intolerant to prior therapy including imatinib."
Effect: modulate
Effect Info: "Dasatinib reduces the levels of p-(Tyr416)-SRC, p-(Ser473)-AKT, p-(Tyr576/577)-FAK, p-(Tyr705)-STAT3, and p-(Tyr1131)-IGF-IR, thereby inhibiting tumors."
Note:
Score: 4.0
Pubmed(PMID): 23580575
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: