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The Development of FAK Inhibitors: A Five-Year Update

Andrea Spallarossa1, Bruno Tasso1, Eleonora Russo1

  • 1Department of Pharmacy, University of Genova, Viale Benedetto XV, 3, 16132 Genova, Italy.

International Journal of Molecular Sciences
|June 24, 2022
PubMed

Insights

Focal adhesion kinase (FAK) inhibitors are crucial for developing new antitumor agents. This review highlights recent FAK-targeting compounds and PROTACs, aiding future cancer drug discovery.

Area of Science:

  • Oncology
  • Biochemistry
  • Medicinal Chemistry

Background:

  • Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase.
  • FAK is over-expressed in various solid cancers.
  • FAK plays a role in tumor development and metastasis.

Purpose of the Study:

  • To review recent FAK inhibitors published since 2017.
  • To discuss compounds with varying potencies and mechanisms of action.
  • To highlight emerging PROTAC molecules targeting FAK.

Main Methods:

  • Literature review of FAK inhibitors and PROTACs.
  • Analysis of compounds published since 2017.
  • Focus on medicinal chemistry aspects.

Main Results:

  • Identification of diverse FAK-blocking compounds.
  • Characterization of different inhibition potencies and mechanisms.
  • Emergence of novel PROTAC molecules for FAK inhibition.

Conclusions:

  • Recent advancements provide new FAK inhibitors for cancer therapy.
  • FAK remains a significant target for antitumor drug development.
  • This review offers insights for future medicinal chemistry investigations.
Keywords:
FAK inhibitorsPROTACanticancer compoundsfocal adhesion kinasemedicinal chemistrypyrimidinestriazines

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