Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors

Simultaneous inhibition of multiple molecular targets is an established strategy to improve the continuance of clinical response to therapy. Here, we screened 49 molecules with dual nanomolar inhibitory activity against BRD4 and PLK1, best classified as dual kinase-bromodomain inhibitors, in pediatr...

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Main Authors: Natalie Timme, Youjia Han, Shuai Liu, Hailemichael O. Yosief, Heathcliff Dorado García, Yi Bei, Filippos Klironomos, Ian C. MacArthur, Annabell Szymansky, Jennifer von Stebut, Victor Bardinet, Constantin Dohna, Annette Künkele, Jana Rolff, Patrick Hundsdörfer, Andrej Lissat, Georg Seifert, Angelika Eggert, Johannes H. Schulte, Wei Zhang, Anton G. Henssen
Format: Article
Language:English
Published: Elsevier 2020-02-01
Series:Translational Oncology
Online Access:http://www.sciencedirect.com/science/article/pii/S1936523319303900