A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Chem Commun (Camb). 2020 May 21;56(41):5532-5535. doi: 10.1039/d0cc00523a. Epub 2020 Apr 16.

Abstract

With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy.

MeSH terms

  • HeLa Cells
  • Humans
  • Ligands
  • Light*
  • Molecular Structure
  • Proteolysis
  • Ubiquitin-Protein Ligases / metabolism*

Substances

  • Ligands
  • Ubiquitin-Protein Ligases