Combination therapy of the EZH2 inhibitor GSK126 and the PARP inhibitor Olaparib shows in vivo synergy in a patient-derived xenograft model of BRCA1-deficient breast cancer
J Puppe, P ter Brugge, M Seressi, O van Tellingen, E van der Burg, U Boon, P Bouwman, P Mallmann, R Schmutzler, M van Lohuizen, J Jonkers · Geburtshilfe und Frauenheilkunde · 2014 · Heft 09
Bibliografische Angaben
Zusammenfassung
Background: Current treatment options for BRCA1-deficient breast cancer are limited highlighting the need for novel targeted therapies. Our group previously demonstrated that EZH2 is overexpressed in BRCA1-deficient breast tumors and a promising target for this subtype. EZH2 is the catalytic subunit of polycomb repressive complex 2 and involved in gene silencing through methylation of histone H3K27. Recently, GSK126, a highly selective inhibitor of EZH2 methyltransferase activity, was discovered. Additionally, PARP inhibitors are effective in breast tumors with defects in homologous recombination due to BRCA1 mu…
