Ricerc@Sapienza

Epigenetic alterations have been associated with both pathogenesis and progression of cancer. By screening of library compounds, we identified a novel hybrid epi-drug MC2884, a HAT/EZH2 inhibitor, able to induce bona fide cancer-selective cell death in both solid and hematological cancers in vitro, ex vivo and in vivo xenograft models. Anticancer action was due to an epigenome modulation by H3K27me3, H3K27ac, H3K9/14ac decrease, and to caspase-dependent apoptosis induction. MC2884 triggered mitochondrial pathway apoptosis by up-regulation of cleaved-BID, and strong down-regulation of BCL2.

Background: Understanding the signalling pathways involved in angiogenesis, and developing anti-angiogenic
drugs are one of the major focuses on cancer research. Herein, we assessed the effect of CPTH6, a lysine
acetyltransferase inhibitor and anti-tumoral compound, on angiogenesis-related properties of both endothelial and
cancer cells.
Methods: The in vitro effect of CPTH6 on protein acetylation and anti-angiogenic properties on endothelial and
lung cancer cells was evaluated via wound healing, trans-well invasion and migration, tube formation,