FAK (PTK2)
FAK is the kinase that tells a cell it is anchored to its surroundings, letting it survive, move and resist drugs. Defactinib, given with the RAF/MEK inhibitor avutometinib, removes that escape route in low-grade serous ovarian cancer; other FAK inhibitors are in trials in meningioma and solid tumours.
Overview
PTK2 (chromosome 8q24.3) encodes focal adhesion kinase 1, a non-receptor tyrosine kinase essential for cell migration, adhesion and spreading, actin reorganisation, the assembly and disassembly of focal adhesions, cell-cycle progression, proliferation and apoptosis; it transduces integrin signals and signals from growth-factor receptors, G protein-coupled receptors, EPHA2, netrin and LDL receptors, and is required for embryonic angiogenesis (UniProt Q05397). In OnCo, FAK is blocked by defactinib in the approved avutometinib-defactinib combination for KRAS-mutant low-grade serous ovarian cancer, where it removes an adhesion-driven escape route from MEK inhibition; by GSK2256098 in meningiomas that have lost the NF2 tumour suppressor merlin and depend on FAK (a synthetic-lethal approach); and by IN10018 in phase 3.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · FAK is the kinase that tells a cell it is anchored to its surroundings, letting it survive, move and resist drugs. Defactinib, given with the RAF/MEK inhibitor avutometinib, removes that escape route in low-grade serous ovarian cancer; other FAK inhibitors are in trials in meningioma and solid tumours.
- 1 · What it is
FAK is the kinase that tells a cell it is anchored to its surroundings, letting it survive, move and resist drugs. Defactinib, given with the RAF/MEK inhibitor avutometinib, removes that escape route in low-grade serous ovarian cancer; other FAK inhibitors are in trials in meningioma and solid tumours.
- 2 · What goes wrong in cancer
The corpus records frame FAK as a resistance node rather than a driver: LGSOC cells arrest and regress only when FAK is blocked alongside RAF-MEK, and NF2-deficient meningioma depends on FAK signalling once merlin is lost.
- 3 · How drugs use it
3 products aim at FAK (PTK2): small molecules. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Biology
The corpus records frame FAK as a resistance node rather than a driver: LGSOC cells arrest and regress only when FAK is blocked alongside RAF-MEK, and NF2-deficient meningioma depends on FAK signalling once merlin is lost.
- Low-grade serous ovarian cancer (defactinib with avutometinib)
- NF2-deficient meningioma (GSK2256098)
- NSCLC, pancreatic, ovarian and small-cell lung cancer (IN10018 trials)
Avutometinib plus defactinib is the first treatment approved specifically for low-grade serous ovarian cancer, a slow-growing type driven by the RAS pathway.
GSK2256098 is a tablet that blocks an enzyme called FAK, which meningiomas missing the NF2 gene rely on. In the Alliance A071401 trial it slowed progression in recurrent NF2-mutant meningiomas, one of the first positive results for a targeted drug in this tumour.
IN10018 is an experimental small-molecule drug from InxMed (Shanghai) in phase 3 trials for non-small-cell lung cancer, pancreatic ductal adenocarcinoma and ovarian cancer, with its target not yet stated publicly.
Notes
top- Prevalence not recorded in this wave: HGNC and UniProt carry no positivity rates and no other source was consulted.
Latest papers
topQuery for this target: (TITLE:"FAK" OR ABSTRACT:"FAK" OR TITLE:"PTK2" OR ABSTRACT:"PTK2" OR TITLE:"FAK1" OR ABSTRACT:"FAK1" OR TITLE:"FADK" OR ABSTRACT:"FADK" OR TITLE:"focal adhesion kinase" OR ABSTRACT:"focal adhesion kinase" OR TITLE:"protein tyrosine kinase 2" OR ABSTRACT:"protein tyrosine kinase 2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about FAK (PTK2), not a curated reading list.
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