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

Chem Commun (Camb)

Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, White City Campus, Wood Lane, London W12 0BZ, UK.

Published: May 2020

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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Source
http://dx.doi.org/10.1039/d0cc00523aDOI Listing

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