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

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

doi:10.1039/d0cc00523a

Public

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

Published in Chemical Communications • Jan 1, 2020

Authors:

Cyrille S. Kounde

Maria M. Shchepinova

Charlie N. Saunders

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 wh...

Subject

Ubiquitin ligase

Degradation (telecommunications)

Chemistry

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