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Issue 41, 2020

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

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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.

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

Supplementary files

Article information


Submitted
20 Jan 2020
Accepted
31 Mar 2020
First published
03 Apr 2020

This article is Open Access

Chem. Commun., 2020,56, 5532-5535
Article type
Communication

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

C. S. Kounde, M. M. Shchepinova, C. N. Saunders, M. Muelbaier, M. D. Rackham, J. D. Harling and E. W. Tate, Chem. Commun., 2020, 56, 5532 DOI: 10.1039/D0CC00523A

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