A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Cyrille S. Kounde, Maria M. Shchepinova, Charlie N. Saunders, Marcel Muelbaier, M.D. Rackham, John D. Harling, Edward W. Tate
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.
Topics & Concepts
Ubiquitin ligaseDegradation (telecommunications)ChemistryLigand (biochemistry)DNA ligaseBiophysicsUbiquitinComputer scienceCombinatorial chemistryBiochemistryBiologyDNAReceptorTelecommunicationsGeneProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysPeptidase Inhibition and Analysis