Id: | acc1772 |
Group: | 2sens |
Protein: | FAK |
Gene Symbol: | PTK2 |
Protein Id: | Q05397 |
Protein Name: | FAK1_HUMAN |
PTM: | phosphorylation |
Site: | Tyr397 |
Site Sequence: | AVSVSETDDYAEIIDEEDTYT |
Disease Category: | Cancer |
Disease: | Myeloma |
Disease Subtype: | multiple myeloma |
Disease Cellline: | MM1 |
Disease Info: | |
Drug: | Palmitoyl-cyclic phosphatidic acid (Pal-cPA) |
Drug Info: | - |
Relation: |
Palmitoyl-cyclic phosphatidic acid (Pal-cPA)
➜
FAK-Tyr397
DOWN
➜
Myeloma
Alleviate
|
Effect: | modulate |
Effect Info: | Drugs inhibit protein phosphorylation and suppress tumor metastasis. |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 12738990 |
Sentence Index: | 12738990_2-3 |
Sentence: | "We demonstrated previously that rat ascites hepatoma MM1 cells require both lysophosphatidic acid (LPA) and fibronectin (FN) for phagokinetic motility and transcellular migration and that these events are regulated through the RhoA-ROCK pathway and tyrosine phosphorylation of proteins including focal adhesion kinase (FAK). Moreover, we reported that palmitoyl-cyclic phosphatidic acid (Pal-cPA), a structural analogue of LPA, inhibits LPA-induced migration of MM1 cells and experimental metastasis of B16 murine melanoma cells." |
Sequence & Structure:
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFIIRPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRERIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDHPHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESKRFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFTSASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWAYDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGYPSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQEIAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLSRGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNEGVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLALRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQMLTAAHALAVDAKNLLDVIDQARLKMLGQTRPH
Select PDB:
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 TargetsPTM Intensity:
source: CPTACPTK2-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: PTMDResidue | 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: DecryptMNo data.
Function score:
source: funscoRNo data.