Available online 29 November 2021
Highlights•Focal adhesion kinase (FAK) is a cytoplasmic protein kinase that is implicated in several cellular functions.
•FAK is an attractive molecular target for cancer therapy.
•Different FAK inhibitors have been developed and tested on in vitro and in vivo models.
•At present, six FAK inhibitors are in clinical trials.
AbstractFocal Adhesion Kinase (FAK) is a 125-kDa cytoplasmic protein kinase that is implicated in several cellular functions. This protein is an attractive molecular target for cancer therapy because a wide variety of studies have demonstrated associations between the activation or elevated expression of FAK and tumor progression, invasion, and drug resistance in malignant tumors. Here, we review the strategies used to inhibit FAK activity in solid tumors. We also include an overview of the preclinical (in vitro and in vivo) and clinical studies on FAK inhibitors.
Keywordsfocal adhesion kinase
FAK
inhibitors
cancer
metastasis
mechanism of action
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