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

Drug Discov Today. 2022 Feb;27(2):664-674. doi: 10.1016/j.drudis.2021.11.025. Epub 2021 Nov 29.

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: Cancer; FAK; Focal adhesion kinase; Inhibitors; Mechanism of action; Metastasis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Focal Adhesion Protein-Tyrosine Kinases / metabolism
  • Humans
  • Neoplasms* / metabolism
  • Protein Kinase Inhibitors* / pharmacology
  • Protein Kinase Inhibitors* / therapeutic use

Substances

  • Protein Kinase Inhibitors
  • Focal Adhesion Protein-Tyrosine Kinases