Issue 12, 2019

PROTAC-mediated crosstalk between E3 ligases

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

Supplementary files

Article information

Article type
Communication
Submitted
30 Nov 2018
Accepted
15 Jan 2019
First published
16 Jan 2019

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

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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