Focal adhesion kinase inhibitors in the treatment of solid tumors: preclinical and clinical evidence

Elsevier

Available online 29 November 2021

Drug Discovery TodayHighlights•

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.

Abstract

Focal 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.

Keywords

focal adhesion kinase

FAK

inhibitors

cancer

metastasis

mechanism of action

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