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Merck

PROTAC-mediated crosstalk between E3 ligases.

Chemical communications (Cambridge, England) (2019-01-24)
Christian Steinebach, Hannes Kehm, Stefanie Lindner, Lan Phuong Vu, Simon Köpff, Álvaro López Mármol, Corinna Weiler, Karl G Wagner, Michaela Reichenzeller, Jan Krönke, Michael Gütschow
PMID30672516
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.