EZH2 inhibition sensitizes BRCA1-deficient breast tumors to the PI3K inhibitor BKM120
J Puppe, M van de Ven, E van der Burg, U Boon, O van Tellingen, P Bouwman, P Mallmann, R Schmutzler, M van Lohuizen, J Jonkers · Geburtshilfe und Frauenheilkunde · 2016 · Heft 10
Bibliografische Angaben
Zusammenfassung
Background: Current treatment options for BRCA1-deficient breast cancer are limited highlighting the need for novel targeted therapies. EZH2 is an epigenetic repressor through its trimethylase activity of H3K27me3 and associated with highly aggressive types of breast cancer. Our group previously demonstrated that EZH2 is overexpressed in BRCA1-deficient breast tumors and a promising target for this subtype. Recently, it was reported that PI3K inhibition is inducing DNA-damage in breast tumors with defects in homologous recombination indicating that the PI3K/ATK signalling pathway is a further attractive target f…