Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells. - Archive ouverte HAL Access content directly
Journal Articles Biochimie Year : 2012

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells.

Abstract

Chemical manipulations undertaken on some bis(bromo- and dibromo-phenol) compounds previously reported by us as wide-spectrum epigenetic inhibitors let us to identify bis (bromo- and dibromo-methoxyphenyl) derivatives highly selective for PR-SET7 and EZH2 (compounds 4, 5, 9, and 10). Western blot analyses were carried out in U937 cells to determine the effects of such compounds on the methyl marks related to the tested enzymes (H3K4me1, H3K9me2, H4H20me1, and H3K27me3). The 1,5-bis(3-bromo-4-methoxyphenyl)penta-1,4-dien-3-one 4 (EC(50) vs EZH2 = 74.9 μM), tested in U937 cells at 50 μM, induced massive cell death and 28% of granulocytic differentiation, highlighting the potential use of EZH2 inhibitors in cancer.
Embargoed file
Embargoed file
Ne sera jamais visible
Loading...

Dates and versions

pasteur-00968696 , version 1 (01-04-2014)

Identifiers

Cite

Sergio Valente, Ilaria Lepore, Carmela Dell'Aversana, Maria Tardugno, Sabrina Castellano, et al.. Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells.. Biochimie, 2012, 94 (11), pp.2308-13. ⟨10.1016/j.biochi.2012.06.003⟩. ⟨pasteur-00968696⟩

Collections

RIIP RIIP_FCB
178 View
1 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More