4.7 Article

PROTAC-mediated crosstalk between E3 ligases

Journal

CHEMICAL COMMUNICATIONS
Volume 55, Issue 12, Pages 1821-1824

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8cc09541h

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Funding

  1. DFG (Emmy-Noether Program) [Kr-3886/2-1, SFB-1074, FOR2372]

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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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