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Recent advances in focal adhesion kinase (FAK)-targeting antitumor agents

Si-Kai Zhu1, Qi Wu2, Guang-Xin Liu2

  • 1Department of Medicinal Chemistry and Pharmaceutic Analysis, School of Pharmacy, The Fourth Military Medical University Changle West Road 169 Xi'an 710032 P. R. China ping_an1718@outlook.com.

RSC Advances
|June 23, 2025
PubMed

Insights

Focal adhesion kinase (FAK) is a key target for cancer drug development. New small molecule inhibitors and proteolysis-targeting chimeras (PROTACs) are being designed to degrade FAK and treat tumors.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase crucial for cell adhesion, survival, and proliferation.
  • Overexpression of FAK is linked to enhanced tumor cell proliferation and migration, making it a significant target in cancer research.
  • The development of targeted therapies against FAK holds great clinical potential for anticancer treatments.

Purpose of the Study:

  • To review the design and biological activity of FAK-targeting antitumor agents.
  • To focus on the chemical structures, antitumor effects, and clinical progress of these agents.
  • To explore novel therapeutic strategies including small molecule inhibitors and PROTACs for FAK-targeted cancer therapy.

Main Methods:

  • Literature review of FAK inhibitors and FAK PROTACs.
  • Analysis of chemical structures and their correlation with biological activity.
  • Evaluation of preclinical and clinical data on FAK-targeting agents.

Main Results:

  • Increasing research on small molecular FAK inhibitors.
  • Development of FAK PROTACs for targeted protein degradation.
  • Identification of promising chemical structures and biological activities for FAK-targeting drugs.

Conclusions:

  • FAK is a validated target for anticancer drug development.
  • Small molecule inhibitors and FAK PROTACs represent promising therapeutic strategies.
  • Further research and clinical trials are essential to advance FAK-targeted therapies for cancer treatment.

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