KAT5 inhibitor

KAT5 inhibitors are a class of epigenetic modulators designed to inhibit the activity of Lysine Acetyltransferase 5 (KAT5), also known as Tip60. KAT5 is the catalytic subunit of the NuA4 histone acetyltransferase complex and is involved in critical cellular functions such as DNA double-strand break repair, transcriptional activation (often in coordination with MYC), and cell cycle regulation. In glioblastoma (GBM), research indicates that KAT5 activity is essential for the transition of tumor stem-like cells between quiescent (G0) and proliferative states. Inhibition of KAT5 has been shown to trap these cells in a G0-like state, characterized by high p27 levels, reduced histone H4 acetylation, and suppressed cell cycle gene expression. This "down-grading" of aggressive tumor cells into a quiescent state represents a potential therapeutic strategy to overcome resistance to standard ablative therapies and improve patient survival in high-grade gliomas.

Other names

Tip60 inhibitorTip-60 inhibitorTip 60 inhibitorNuA4 complex inhibitorNuA-4 complex inhibitorNuA 4 complex inhibitor