Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2)

J Med Chem. 2023 Jul 27;66(14):9445-9465. doi: 10.1021/acs.jmedchem.2c01859. Epub 2023 Jul 14.

Abstract

Tissue transglutaminase (TG2) is a multifunctional enzyme involved in the cross-linking of extracellular matrix proteins, formation of complexes with fibronectin (FN) and integrins, and GTP hydrolysis. TG2 is activated in several pathological conditions, including cancer. We recently described a novel series of ligands that bind to TG2 and inhibit its interaction with FN. Because TG2 acts via multiple mechanisms, we set out to pursue a targeted protein degradation strategy to abolish TG2's myriad functions. Here, we report the synthesis and characterization of a series of VHL-based degraders that reduce TG2 in ovarian cancer cells in a proteasome-dependent manner. Degradation of TG2 resulted in significantly reduced cancer cell adhesion and migration in vitro in scratch-wound and migration assays. These results strongly indicate that further development of more potent and in vivo efficient TG2 degraders could be a new strategy for reducing the dissemination of ovarian and other cancers.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cell Adhesion
  • Female
  • GTP-Binding Proteins / metabolism
  • Humans
  • Protein Glutamine gamma Glutamyltransferase 2*
  • Proteolysis Targeting Chimera
  • Transglutaminases*

Substances

  • Protein Glutamine gamma Glutamyltransferase 2
  • Transglutaminases
  • Proteolysis Targeting Chimera
  • GTP-Binding Proteins