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Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity.

Eriko Koide1, Mikaela L Mohardt1, Zainab M Doctor1,2

  • 1Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA.

Chembiochem : a European Journal of Chemical Biology
|April 23, 2023
PubMed
Summary

Targeting focal adhesion kinase (FAK) via degradation, not just inhibition, shows improved cancer cell activity. New tools, BSJ-04-175 and BSJ-04-146, enable detailed study of FAK

Keywords:
PROTACcancerdegradersfocal adhesion kinaseinhibitors

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Focal adhesion kinase (FAK) is overexpressed in cancer and crucial for cellular processes.
  • Current FAK inhibitors targeting kinase activity have shown limited clinical efficacy as single agents.
  • Targeting FAK offers a promising therapeutic strategy for cancer treatment.

Purpose of the Study:

  • To develop and characterize novel chemical tools for FAK inhibition and degradation.
  • To evaluate the comparative efficacy of FAK inhibition versus FAK degradation in cancer models.
  • To dissect the downstream signaling consequences of abolishing FAK activity.

Main Methods:

  • Structure-guided design of a selective FAK inhibitor (BSJ-04-175) and degrader (BSJ-04-146).
  • Assessment of FAK degradation potency, specificity, and durability in cancer cells and in vivo.
  • Analysis of downstream signaling pathways and cellular phenotypes (viability, migration) in response to FAK modulation.

Main Results:

  • BSJ-04-146 achieved rapid, potent, and specific FAK degradation in cancer cells with durable effects in mice.
  • FAK degradation demonstrated superior efficacy compared to kinase inhibition in modulating downstream signaling.
  • Targeted FAK degradation significantly improved outcomes in cancer cell viability and migration assays.

Conclusions:

  • Targeted protein degradation of FAK offers advantages over traditional kinase inhibition for cancer therapy.
  • BSJ-04-175 and BSJ-04-146 serve as valuable chemical probes for investigating FAK biology.
  • These findings support further development of FAK degraders as a novel therapeutic approach for cancer.