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PROTAC-mediated crosstalk between E3 ligases

Author:
SteinebachThese authors contributed equally., Christian, Kehm, Hannes, Lindner, Stefanie, Vu, Lan Phuong, Köpff, Simon, López Mármol, Álvaro, Weiler, Corinna, Wagner, Karl G., Reichenzeller, Michaela, Krönke, Jan, Gütschow, Michael
Source:
Chemical communications 2019 v.55 no.12 pp. 1821-1824
ISSN:
1364-548X
Subject:
chemical communication, chimerism, dimerization, ligands, ligases, protein content, proteolysis
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.
Agid:
6302186