IMR Press / FBL / Volume 19 / Issue 4 / DOI: 10.2741/4236

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Review
Targeting FAK in human cancer: from finding to first clinical trials
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1 Department of Surgical Oncology, Roswell Park Cancer Institute, Buffalo, NY, USA
Academic Editor:Vita M. Golubovskaya
Front. Biosci. (Landmark Ed) 2014, 19(4), 687–706;
Published: 1 January 2014
(This article belongs to the Special Issue Focal adhesion signaling in cancer)

It is twenty years since Focal Adhesion Kinase (FAK) was found to be overexpressed in many types of human cancer. FAK plays an important role in adhesion, spreading, motility, invasion, metastasis, survival, angiogenesis, and recently has been found to play an important role as well in epithelial to mesenchymal transition (EMT), cancer stem cells and tumor microenvironment. FAK has kinase-dependent and kinase independent scaffolding, cytoplasmic and nuclear functions. Several years ago FAK was proposed as a potential therapeutic target; the first clinical trials were just reported, and they supported further studies of FAK as a promising therapeutic target. This review discusses the main functions of FAK in cancer, and specifically focuses on recent novel findings on the role of FAK in cancer stem cells, microenvironment, epithelial-to-mesenchymal transition, invasion, metastasis, and also highlight new approaches of targeting FAK and critically discuss challenges that lie ahead for its targeted therapeutics. The review provides a summary of translational approaches of FAK-targeted and combination therapies and outline perspectives and future directions of FAK research.

Focal Adhesion Kinase
Small molecule inhibitors
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