2. Academic Validation
  3. PROTAC-mediated crosstalk between E3 ligases

PROTAC-mediated crosstalk between E3 ligases

  • Chem Commun (Camb). 2019 Feb 5;55(12):1821-1824. doi: 10.1039/c8cc09541h.
Christian Steinebach 1,  Hannes Kehm,  Stefanie Lindner,  Lan Phuong Vu,  Simon Köpff,  Álvaro López Mármol,  Corinna Weiler,  Karl G Wagner,  Michaela Reichenzeller,  Jan Krönke,  Michael Gütschow
Affiliations

Affiliation

  • 1 Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany. [email protected].
PMID: 30672516 DOI: 10.1039/c8cc09541h
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.

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