| Tchem | Focal adhesion kinase 1 |
This gene encodes a cytoplasmic protein tyrosine kinase which is found concentrated in the focal adhesions that form between cells growing in the presence of extracellular matrix constituents. The encoded protein is a member of the FAK subfamily of protein tyrosine kinases but lacks significant sequence similarity to kinases from other subfamilies. Activation of this gene may be an important early step in cell growth and intracellular signal transduction pathways triggered in response to certain neural peptides or to cell interactions with the extracellular matrix. Several transcript variants encoding different isoforms have been found for this gene, but the full-length natures of only four of them have been determined. [provided by RefSeq, Oct 2015]
Comments
Property Summary
| NCBI Gene PubMed Count | 668 |
| Grant Count | 967 |
| R01 Count | 686 |
| Funding | $66,766,697.08 |
| PubMed Score | 956.94 |
| PubTator Score | 1563.61 |
| Disease | log2 FC | p |
|---|---|---|
| oligodendroglioma | 1.400 | 0.001 |
| osteosarcoma | 3.008 | 0.000 |
| pancreatic ductal adenocarcinoma liver m... | 1.598 | 0.001 |
| non-small cell lung cancer | 1.474 | 0.000 |
| intraductal papillary-mucinous adenoma (... | 1.900 | 0.000 |
| intraductal papillary-mucinous carcinoma... | 2.100 | 0.001 |
| intraductal papillary-mucinous neoplasm ... | 1.900 | 0.004 |
| subependymal giant cell astrocytoma | -1.974 | 0.005 |
| spina bifida | -2.555 | 0.039 |
| Pick disease | -1.200 | 0.000 |
| mucosa-associated lymphoid tissue lympho... | 1.093 | 0.005 |
| ovarian cancer | 2.500 | 0.000 |
| Breast cancer | 1.100 | 0.000 |
CHEMBL207084
pIC50 7.54
CHEMBL3657336
pIC50 7.54
CHEMBL3657327
pIC50 7.54
CHEMBL3657375
pIC50 7.55
CHEMBL3665937
pIC50 7.57
CHEMBL3657314
pIC50 7.59
CHEMBL3657301
pIC50 7.59
CHEMBL3665876
pIC50 7.60
CHEMBL1934343
pIC50 7.60
CHEMBL3692186
pIC50 7.60
CHEMBL2315584
pKd 7.62
CHEMBL2315583
pKd 7.62
CHEMBL3692203
pIC50 7.64
CHEMBL3692204
pIC50 7.64
CHEMBL3642416
pIC50 7.66
CHEMBL3692180
pIC50 7.68
CHEMBL1934334
pIC50 7.68
CHEMBL1934339
pIC50 7.68
CHEMBL3665907
pIC50 7.70
CHEMBL3692191
pIC50 7.70
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 727 | screening |
811 / 0 / 96078 | Primary biochemical high-throughput screening assay for inhibitors of Focal Adhesion Kinase (FAK) |
| 794 | other |
212 / 0 / 541 | Confirmation biochemical assay for inhibitors of Focal Adhesion Kinase (FAK) |
| 810 | confirmatory |
110 / 0 / 100 | Dose-response biochemical assay for inhibitors of Focal Adhesion Kinase (FAK) |
| 1802 | summary |
0 / 0 / 0 | Summary of probe development efforts to identify inhibitors of Focal Adhesion Kinase (FAK) |
| 1982 | other |
0 / 0 / 0 | Kinase inhibition selectivity assay for compound SID-48409448 |
| PMID | Text |
|---|---|
| 27009091 | CEP-37440 decreased the cell proliferation of FC-IBC02, SUM190, and KPL4 by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397). |
| 26992741 | Our findings suggest that the targets of FAK play a key role in metastasis |
| 26975850 | Increased focal adhesion kinase(FAK)activity. |
| 26962872 | Combining erlotinib with FAK inhibitor was also potent in vivo as evidenced by reduced tumor growth in the A549 mouse xenograft model. |
| 26956728 | Bit1 may be an important regulator in cell growth, apoptosis, migration and invasion of esophageal squamous cell carcinoma via targeting FAK-paxillin pathway. |
| 26944318 | In clinical samples of hepatocellular carcinom (HCC), miR-379-5p negatively correlated with FAK, which was up-regulated in HCC. |
| 26923073 | Collectively, our data demonstrate that DCMF induces cell migration and promotes wound healing through activation of Src/FAK, ERK, AKT, and p38 MAPK signaling. |
| 26895766 | Data suggest that, in colonic/prostatic neoplasm cells, increased expression of NDRG1 decreases activating phosphorylation of FAK and paxillin; silencing/inhibition of NDRG1 results in opposite effect and inhibits neoplasm cell migration/adhesion. |
| 26892465 | Data suggest that simultaneous targeting of mammalian target of rapamycin (mTOR)- and adhesion kinase (FAK)-related pathways might offer a strategy for treating acute lymphoblastic leukemia (ALL). |
| 26833789 | Modulation of FAK and Src adhesion signaling occurs independently of adhesion complex composition. |
| More... |
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQK 1 - 70 IVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTED 71 - 140 KPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKS 141 - 210 LLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGI 211 - 280 SYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRL 281 - 350 VNGTSQSFIIRPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRE 351 - 420 RIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDHPHIVKLIGVI 421 - 490 TENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESKRFVHRDIAARNVLVSSNDCV 491 - 560 KLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFTSASDVWMFGVCMWEILMHGVKPFQGVKNND 561 - 630 VIGRIENGERLPMPPNCPPTLYSLMTKCWAYDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQAT 631 - 700 VSWDSGGSDEAPPKPSRPGYPSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQ 701 - 770 TDSWNHRPQEIAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLS 771 - 840 RGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNEGVKLQPQEIS 841 - 910 PPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLALRTLLATVDETIPLLPASTH 911 - 980 REIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQMLTAAHALAVDAKNLLDVIDQARLKMLGQTR 981 - 1050 PH 1051 - 1052 //
| PMID | Year | Title |
|---|---|---|
| 27009091 | 2016 | The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. |
| 26992741 | 2016 | Ling Zhi-8 reduces lung cancer mobility and metastasis through disruption of focal adhesion and induction of MDM2-mediated Slug degradation. |
| 26975850 | 2016 | Loss of miR-203 regulates cell shape and matrix adhesion through ROBO1/Rac/FAK in response to stiffness. |
| 26962872 | 2016 | Focal Adhesion Kinase Inhibitors in Combination with Erlotinib Demonstrate Enhanced Anti-Tumor Activity in Non-Small Cell Lung Cancer. |
| 26956728 | 2016 | Bit1 knockdown contributes to growth suppression as well as the decreases of migration and invasion abilities in esophageal squamous cell carcinoma via suppressing FAK-paxillin pathway. |
| 26944318 | 2016 | MicroRNA-379-5p inhibits tumor invasion and metastasis by targeting FAK/AKT signaling in hepatocellular carcinoma. |
| 26923073 | 2016 | A synthetic isoflavone, DCMF, promotes human keratinocyte migration by activating Src/FAK signaling pathway. |
| 26895766 | 2016 | Targeting the Metastasis Suppressor, N-Myc Downstream Regulated Gene-1, with Novel Di-2-Pyridylketone Thiosemicarbazones: Suppression of Tumor Cell Migration and Cell-Collagen Adhesion by Inhibiting Focal Adhesion Kinase/Paxillin Signaling. |
| 26892465 | 2016 | Synergism between the mTOR inhibitor rapamycin and FAK down-regulation in the treatment of acute lymphoblastic leukemia. |
| 26833789 | 2016 | Modulation of FAK and Src adhesion signaling occurs independently of adhesion complex composition. |
| More... |
