Id: acc3687
Group: 1sens
Protein: FAK
Gene Symbol: PTK2
Protein Id: Q05397
Protein Name: FAK1_HUMAN
PTM: phosphorylation
Site: Tyr
Site Sequence:
Disease Category: Cancer
Disease: Hepatocellular Carcinoma
Disease Subtype:
Disease Cellline: SMMC-7721
Disease Info:
Drug: TGF-β1
Drug Info: "TGF-β1 is a cytokine that plays a crucial role in various biological processes such as cell growth, differentiation, and immune regulation."
Effect: modulate
Effect Info: TGF-β1 signaling can regulate key signaling pathways in hepatocellular carcinoma cells by modulating the phosphorylation of Akt and FAK and relying on the cell adhesion mechanism.
Note:
Score: 4.0
Pubmed(PMID): 14637150
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

No intensity data of this site,
show all other sites!

PTK2-Ser29
Cancer Intensity
BRCA -2.43
COAD
HGSC 0.863
ccRCC 0.19
GBM 0.396
HNSC 0.598
LUAD 0.118
LUSC 0.436
non_ccRCC 0.958
PDAC -0.426
UCEC -0.703
PTK2-Ser390
Cancer Intensity
BRCA
COAD 0.882
HGSC -1.086
ccRCC
GBM 0.204
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2-Ser392
Cancer Intensity
BRCA
COAD
HGSC -0.683
ccRCC
GBM 0.311
HNSC 0.961
LUAD -1.376
LUSC
non_ccRCC
PDAC
UCEC 0.788
PTK2-Ser568
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2-Ser702
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.863
GBM
HNSC
LUAD 0.233
LUSC
non_ccRCC
PDAC -1.096
UCEC
PTK2-Ser705
Cancer Intensity
BRCA 1.692
COAD
HGSC
ccRCC
GBM
HNSC 0.067
LUAD -0.651
LUSC -0.337
non_ccRCC
PDAC -0.772
UCEC
PTK2-Ser708
Cancer Intensity
BRCA 1.97
COAD 0.049
HGSC
ccRCC 0.154
GBM
HNSC 0.406
LUAD -0.561
LUSC -0.32
non_ccRCC
PDAC -1.581
UCEC -0.117
PTK2-Ser716
Cancer Intensity
BRCA
COAD -1.009
HGSC
ccRCC 0.14
GBM 0.356
HNSC 1.419
LUAD
LUSC
non_ccRCC
PDAC
UCEC -0.907
PTK2-Ser722
Cancer Intensity
BRCA
COAD -0.265
HGSC 2.089
ccRCC
GBM 0.333
HNSC
LUAD -0.894
LUSC
non_ccRCC -0.375
PDAC -0.199
UCEC -0.689
PTK2-Ser840
Cancer Intensity
BRCA
COAD 1.141
HGSC
ccRCC -0.13
GBM
HNSC 0.246
LUAD 0.299
LUSC -0.2
non_ccRCC
PDAC 0.659
UCEC -2.014
PTK2-Ser843
Cancer Intensity
BRCA
COAD 0.028
HGSC
ccRCC -0.136
GBM 1.188
HNSC 0.169
LUAD 0.224
LUSC 0.928
non_ccRCC
PDAC -0.267
UCEC -2.135
PTK2-Ser850
Cancer Intensity
BRCA
COAD 0.344
HGSC
ccRCC -1.085
GBM
HNSC -0.475
LUAD 1.216
LUSC
non_ccRCC
PDAC
UCEC
PTK2-Ser910
Cancer Intensity
BRCA 1.569
COAD -0.212
HGSC
ccRCC -0.358
GBM -0.058
HNSC 0.662
LUAD -0.174
LUSC 0.71
non_ccRCC -1.419
PDAC 0.888
UCEC -1.609
PTK2-Thr394
Cancer Intensity
BRCA
COAD -0.36
HGSC -1.442
ccRCC
GBM 0.277
HNSC 0.237
LUAD
LUSC
non_ccRCC
PDAC
UCEC 1.288
PTK2-Thr575
Cancer Intensity
BRCA
COAD
HGSC -1.145
ccRCC 0.703
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.442
PTK2-Thr914
Cancer Intensity
BRCA
COAD 0.707
HGSC
ccRCC
GBM
HNSC -0.707
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2-Tyr397
Cancer Intensity
BRCA
COAD 0.587
HGSC -1.155
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.567
PTK2-Tyr570
Cancer Intensity
BRCA -0.018
COAD 0.395
HGSC 1.385
ccRCC 0.37
GBM -0.571
HNSC -0.744
LUAD -1.592
LUSC -0.966
non_ccRCC 0.897
PDAC 1.49
UCEC -0.646
PTK2-Tyr576
Cancer Intensity
BRCA
COAD 0.473
HGSC 1.142
ccRCC
GBM -0.517
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC -1.098
PTK2-Tyr577
Cancer Intensity
BRCA
COAD 1.045
HGSC
ccRCC
GBM -0.097
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC -0.948
PTK2-Tyr720
Cancer Intensity
BRCA
COAD -0.364
HGSC 1.575
ccRCC
GBM 0.353
HNSC
LUAD -0.64
LUSC
non_ccRCC
PDAC
UCEC -0.923
PTK2-Tyr861
Cancer Intensity
BRCA
COAD 0.904
HGSC
ccRCC
GBM -1.074
HNSC 0.17
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2-Tyr925
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.981
GBM 0.023
HNSC
LUAD 0.293
LUSC 0.993
non_ccRCC 0.192
PDAC -1.892
UCEC -0.59
PTK2B-Ser361
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD 0.707
LUSC -0.707
non_ccRCC
PDAC
UCEC
PTK2B-Ser375
Cancer Intensity
BRCA 0.873
COAD -0.141
HGSC 2.388
ccRCC -0.73
GBM -0.066
HNSC -0.489
LUAD 0.023
LUSC 0.434
non_ccRCC -0.383
PDAC -1.494
UCEC -0.416
PTK2B-Ser571
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Ser746
Cancer Intensity
BRCA
COAD -0.625
HGSC
ccRCC
GBM 1.153
HNSC -0.528
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Ser747
Cancer Intensity
BRCA
COAD -0.707
HGSC
ccRCC
GBM
HNSC 0.707
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Ser758
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 1.122
GBM -0.326
HNSC -0.796
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Ser762
Cancer Intensity
BRCA
COAD -0.33
HGSC
ccRCC -0.021
GBM -0.325
HNSC -0.996
LUAD 1.671
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Ser778
Cancer Intensity
BRCA 0.482
COAD -0.158
HGSC 2.376
ccRCC -0.259
GBM -0.528
HNSC -0.202
LUAD -0.526
LUSC 0.229
non_ccRCC 0.124
PDAC -1.539
UCEC
PTK2B-Ser839
Cancer Intensity
BRCA
COAD
HGSC 1.459
ccRCC -1.431
GBM -0.527
HNSC -0.162
LUAD -0.059
LUSC 0.72
non_ccRCC
PDAC
UCEC
PTK2B-Thr842
Cancer Intensity
BRCA 1.307
COAD -0.496
HGSC
ccRCC 0.037
GBM -1.372
HNSC -0.652
LUAD 1.788
LUSC 0.167
non_ccRCC
PDAC -0.067
UCEC -0.713
PTK2B-Tyr579
Cancer Intensity
BRCA 0.707
COAD
HGSC
ccRCC
GBM -0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Tyr580
Cancer Intensity
BRCA 0.707
COAD
HGSC
ccRCC
GBM -0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Tyr756
Cancer Intensity
BRCA
COAD 0.248
HGSC
ccRCC
GBM 0.853
HNSC -1.101
LUAD
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Tyr834
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.605
GBM -1.154
HNSC
LUAD 0.549
LUSC
non_ccRCC
PDAC
UCEC
PTK2B-Tyr849
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM -0.707
HNSC
LUAD
LUSC 0.707
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - U Uterine serous carcinoma Phosphorylation 36409196
- - U Cervical cancer/carcinoma Phosphorylation 24058594
- - U Hepatocellular carcinoma/hepatocarcinoma/hepatoma Phosphorylation 11287749
- - U Breast cancer Phosphorylation 12421874
- - U Head and neck squamous cell carcinoma Phosphorylation 22483702
- - U Ovarian cancer Phosphorylation 36217544
- - U Cancer Phosphorylation 36656716

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 Tyr570 Y(ph)MEDSTYYK PC-9 AZD4547 7.7576 -
Q05397 PTK2 P Tyr720 QATVSWDSGGSDEAPPKPSRPGY(ph)PSPR PC-9 AZD4547 7.2101 -
Q05397 PTK2 P Tyr720 RQATVSWDSGGSDEAPPKPSRPGY(ph)PSPR PC-9 AZD4547 7.1997 -
Q05397 PTK2 P Ser574;Thr575;Tyr576;Tyr577 YMEDS(ph)T(ph)Y(ph)Y(ph)K PC-9 AZD4547 1.5229 -
Q05397 PTK2 P Tyr570 Y(ph)MEDSTYYK PC-9 Gefitinib 8.1192 -
Q05397 PTK2 P Tyr576 YMEDSTY(ph)YK PC-9 Gefitinib 4.9948 -
Q05397 PTK2 P Tyr720 RQATVSWDSGGSDEAPPKPSRPGY(ph)PSPR PC-9 GeftinibAZD4547-1to80 9.855 -
Q05397 PTK2 P Tyr570 Y(ph)MEDSTYYK PC-9 GeftinibAZD4547-1to80 8.4574 -
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: