A caged E3 ligase ligand for PROTAC-mediated protein degradation with light. Issue 41 (16th April 2020) - Kounde, Cyrille S.
Abstract : Caging of a widely used Von Hippel Lindau E3 ligase ligand for targeted protein degradation with PROTACs allows light-activated proteolysis. 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.