Id: | acc5039 |
Group: | 1sens |
Protein: | FAK |
Gene Symbol: | PTK2 |
Protein Id: | Q05397 |
Protein Name: | FAK1_HUMAN |
PTM: | phosphorylation |
Site: | Tyr577 |
Site Sequence: | SRYMEDSTYYKASKGKLPIKW |
Disease Category: | Eye diseases |
Disease: | Neovascular Eye Disease |
Disease Subtype: | |
Disease Cellline: | HUVECs |
Disease Info: | |
Drug: | Curcumolide |
Drug Info: | Curcumolide is a compound with potential pharmacological activities. It may have certain effects on specific physiological processes and is an object of research in the field of pharmacology. |
Effect: | modulate |
Effect Info: | "Curcumolide can inhibit the phosphorylation of VEGFR2, thereby suppressing the phosphorylation of multiple downstream proteins and inhibiting the formation of retinal neovascularization. It may be a potential candidate drug for the treatment of proliferative diabetic retinopathy." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 31450226 |
Sentence Index: | 31450226_10 |
Sentence: | Intravitreal injection of curcumolide reduced the formation of retinal neovascular tufts and VEGFR2 phosphorylation in the murine OIR model at concentrations administered without definite cellular and retinal toxicities. |
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-Tyr577 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | 1.045 |
HGSC | |
ccRCC | |
GBM | -0.097 |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | -0.948 |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
Y | 577 | D | Hepatocellular carcinoma | Phosphorylation | 36209205 |
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: DecryptMProtein | Gene | PTM | Position | Modified sequence | Cell | Drug | pEC50 | Regulation | Experiment |
---|---|---|---|---|---|---|---|---|---|
Q05397 | PTK2 | P | Ser574;Thr575;Tyr576;Tyr577 | YMEDS(ph)T(ph)Y(ph)Y(ph)K | PC-9 | AZD4547 | 1.5229 | - |
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: funscoRNo data.