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Issue 12, 2019
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PROTAC-mediated crosstalk between E3 ligases

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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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Publication details

The article was received on 30 Nov 2018, accepted on 15 Jan 2019 and first published on 16 Jan 2019


Article type: Communication
DOI: 10.1039/C8CC09541H
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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