Issue 12, 2019
From the journal:

Chemical Communications

PROTAC-mediated crosstalk between E3 ligases†

Christian Steinebach, ORCID logo ‡a   Hannes Kehm,‡b   Stefanie Lindner,b   Lan Phuong Vu,a   Simon Köpff,b   Álvaro López Mármol,c   Corinna Weiler,a   Karl G. Wagner,c   Michaela Reichenzeller,bd   Jan Krönke ORCID logo *b  and  Michael Gütschow ORCID logo *a  

* Corresponding authors

a Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany
E-mail: guetschow@uni-bonn.de

b Department of Internal Medicine III, University Hospital Ulm, Albert-Einstein-Allee 23, 89081 Ulm, Germany
E-mail: jan.kroenke@uni-ulm.de

c Pharmaceutical Institute, Pharmaceutical Technology, University of Bonn, Gerhard-Domagk-Straße 3, 53121 Bonn, Germany

d DKFZ, Molecular Genetics, Im Neuenheimer Feld 260, 69120 Heidelberg, Germany

Abstract

Small-molecule heterobifunctional degraders can effectively control protein levels and are useful research tools. We assembled proteolysis targeting chimeras (PROTACs) from a cereblon (CRBN) and a von-Hippel-Lindau (VHL) ligase ligand and demonstrated a PROTAC-induced heterodimerization of the two E3 ligases leading to unidirectional and efficient degradation of CRBN.

Graphical abstract: PROTAC-mediated crosstalk between E3 ligases

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Article information

DOI
https://doi.org/10.1039/C8CC09541H
Article type
Communication
Submitted
30 Nov 2018
Accepted
15 Jan 2019
First published
16 Jan 2019

Chem. Commun., 2019,55, 1821-1824

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PROTAC-mediated crosstalk between E3 ligases

C. Steinebach, H. Kehm, S. Lindner, L. P. Vu, S. Köpff, Á. López Mármol, C. Weiler, K. G. Wagner, M. Reichenzeller, J. Krönke and M. Gütschow, Chem. Commun., 2019, 55, 1821 DOI: 10.1039/C8CC09541H

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