PROTAC-mediated crosstalk between E3 ligases.

Autor: 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
Předmět:
Zdroj: Chemical Communications; 2/11/2019, Vol. 55 Issue 12, p1821-1824, 4p
Abstrakt: 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]
Databáze: Complementary Index