Targeting focal adhesion kinase: From molecular mechanisms to next-generation cancer therapeutics - PubMed
7 hours ago
- #Cancer Therapeutics
- #Molecular Mechanisms
- #FAK
- Focal adhesion kinase (FAK) is a cytoplasmic tyrosine kinase crucial for cell migration, metastasis, growth, and survival.
- FAK modulates oncogenic pathways like PI3K/AKT and Ras/ERK through autophosphorylation at Y397.
- FAK is overexpressed in solid tumors and correlates with tumor stage, metastasis, and poor prognosis.
- FAK promotes tumor malignancy by inducing EMT, chemoresistance, and stemness properties.
- Targeting FAK is challenging due to signal complexity; only eight small-molecule inhibitors have reached clinical trials.
- New strategies like PROTAC degraders, PPI blockers, allosteric inhibitors, and natural products show promise.
- The review covers FAK's structure, regulatory mechanisms, role in tumors, and inhibitor development.