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

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

Chemical communications (Cambridge, England) (2020-04-17)
Cyrille S Kounde, Maria M Shchepinova, Charlie N Saunders, Marcel Muelbaier, Mark D Rackham, John D Harling, Edward W Tate
PMID32297626
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.