Design, Synthesis, and Biological Evaluation of MEK PROTACs

PROteolysis TArgeting Chimeras (PROTACs) targeting the degradation of MEK have been designed based on allosteric MEK inhibitors. Inhibition of the phosphorylation of ERK1/2 was less effective with the PROTACs than a small-molecule inhibitor; the best PROTACs, however, were more effective in inhibiti...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Journal of medicinal chemistry 2020-01, Vol.63 (1), p.157-162
Hauptverfasser: Vollmer, Stefan, Cunoosamy, Danen, Lv, Huafei, Feng, Huanxi, Li, Xia, Nan, Ziyang, Yang, Wenzhen, Perry, Matthew W. D
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:PROteolysis TArgeting Chimeras (PROTACs) targeting the degradation of MEK have been designed based on allosteric MEK inhibitors. Inhibition of the phosphorylation of ERK1/2 was less effective with the PROTACs than a small-molecule inhibitor; the best PROTACs, however, were more effective in inhibiting proliferation of A375 cells than an inhibitor.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.9b00810