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Updated: Oct 27, 2025

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library

Published on: September 30, 2019

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Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy

Xiao-Jing Pang1, Xiu-Juan Liu1, Yuan Liu1

  • 1Key Laboratory of Advanced Drug Preparation Technologies (Ministry of Education), Institute of Drug Discovery & Development, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.

Molecules (Basel, Switzerland)
|July 24, 2021
PubMed

Insights

Focal adhesion kinase (FAK) is a key target in cancer therapy. This review summarizes FAK inhibitors and degraders, including those in clinical trials, offering insights for developing new anticancer agents.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Focal adhesion kinase (FAK) is a nonreceptor tyrosine kinase crucial for cell functions.
  • FAK overexpression is linked to enhanced tumor growth, migration, and survival in various cancers.
  • Targeting FAK with small molecules represents a promising therapeutic strategy.

Purpose of the Study:

  • To review the structure and biological function of FAK.
  • To summarize the design, chemical types, and activity of FAK inhibitors.
  • To provide a reference for the discovery of novel anticancer agents targeting FAK.

Main Methods:

  • Literature review of FAK inhibitors and degraders.
  • Analysis of FAK inhibitors currently in clinical trials (e.g., GSK-2256098, VS-6063).
  • Exploration of FAK degraders developed using proteolysis targeting chimera (PROTAC) technology.

Main Results:

  • FAK inhibitors have demonstrated anticancer activity through various mechanisms.
  • Six FAK inhibitors are currently in clinical trials, indicating significant therapeutic potential.
  • FAK degraders offer a novel approach to FAK-targeted cancer therapy.

Conclusions:

  • FAK plays a critical role in cancer progression, making it a viable therapeutic target.
  • The development of FAK inhibitors and degraders is advancing cancer treatment strategies.
  • This review consolidates current knowledge on FAK-targeted therapies for future drug discovery.
Keywords:
PROTACanticancer activitydiaminopyrimidinesfocal adhesion kinasetriazine

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