Selective and Potent PROTAC Degraders of c-Src Kinase

ACS Chem Biol. 2024 Jan 19;19(1):110-116. doi: 10.1021/acschembio.3c00548. Epub 2023 Dec 19.

Abstract

Using dasatinib linked to E3 ligase ligands, we identified a potent and selective dual Csk/c-Src PROTAC degrader. We then replaced dasatinib, the c-Src-directed ligand, with a conformation-selective analogue that stabilizes the αC-helix-out conformation of c-Src. Using the αC-helix-out ligand, we identified a PROTAC that is potent and selective for c-Src. We demonstrated a high degree of catalysis with our c-Src PROTACs. Using our c-Src PROTACs, we identified pharmacological advantages of c-Src degradation compared to inhibition with respect to cancer cell proliferation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • CSK Tyrosine-Protein Kinase / metabolism
  • Cell Proliferation
  • Dasatinib / pharmacology
  • Ligands
  • Proteolysis
  • Ubiquitin-Protein Ligases* / metabolism

Substances

  • Dasatinib
  • CSK Tyrosine-Protein Kinase
  • Ligands
  • Ubiquitin-Protein Ligases