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

Cyrille S. Kounde,Maria M. Shchepinova,Charlie N. Saunders,Marcel Muelbaier,Mark D. Rackham,John D. Harling,Edward W. Tate

CHEMICAL COMMUNICATIONS（2020）

Cited 77|Views25

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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.

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