PROTAC-mediated crosstalk between E3 ligases.
- Resource Type
- Article
- Authors
- Steinebach, 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. 2/11/2019, Vol. 55 Issue 12, p1821-1824. 4p.
- Subject
- *VON Hippel-Lindau disease
*CHEMICAL reactions
*UBIQUITIN ligases
- Language
- ISSN
- 1359-7345
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. [ABSTRACT FROM AUTHOR]