G4-PROTAC: targeted degradation of a G-quadruplex binding protein

Chem Commun (Camb). 2021 Nov 30;57(95):12816-12819. doi: 10.1039/d1cc05025g.

Abstract

G-quadruplex (G4) binding proteins regulate important biological processes, but their interaction networks are poorly understood. We report the first use of G4 as a warhead of a proteolysis-targeting chimera (G4-PROTAC) for targeted degradation of a G4-binding protein (RHAU/DHX36). G4-PROTAC provides a new way to explore G4-protein networks and to develop potential therapeutics.

MeSH terms

  • DEAD-box RNA Helicases / chemistry
  • DEAD-box RNA Helicases / metabolism*
  • G-Quadruplexes
  • Humans
  • Proteolysis

Substances

  • DHX36 protein, human
  • DEAD-box RNA Helicases