Histone deacetylase inhibitors, anticancerous mechanism and therapy for gastrointestinal cancers.

Histone acetylation regulates gene transcription. Histone acetylation is a reversible process: histone acetyltransferases (HAT) transfer the acetyl moiety from acetyl coenzyme A to the lysine, and histone deacetylases (HDAC) remove the acetyl groups re-establishing the positive charge in the histones. HDAC inhibitors have antiproliferative activity against human cancer cells via cell cycle arrest, pro-differentiation, and pro-apoptosis. In recent years, many studies have shown that specific HDAC inhibitors are helpful for gastrointestinal cancer therapy.