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

doi:10.1039/D0CC00523A

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

Cyrille S. Kounde,

^a Maria M. Shchepinova,^a Charlie N. Saunders,

^a Marcel Muelbaier,

^b Mark D. Rackham,^c John D. Harling

^d and Edward W. Tate

*^a

Author affiliations

* Corresponding authors

^a Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, White City Campus, Wood Lane, London W12 0BZ, UK
E-mail: e.tate@imperial.ac.uk

^b Cellzome GmbH, a GSK Company, Meyerhofstrasse 1, 69117 Heidelberg, Germany

^c Merck Sharp & Dohme, 1st Floor, 2 Pancras Square, London NC1 4AG, UK

^d GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK

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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Article information

DOI: https://doi.org/10.1039/D0CC00523A
Article type: Communication
Submitted: 20 Jan 2020
Accepted: 31 Mar 2020
First published: 03 Apr 2020
This article is Open Access

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Chem. Commun., 2020,56, 5532-5535

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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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Chemical Communications

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

Abstract

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

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