HDAC inhibitor

Histone deacetylases (HDACs), that may be called protein deacetylases (PDAC) as some of their targets are non-histone proteins, are a family of eleven zinc-dependent enzymes that have gained major interest as therapeutic targets, mainly in cancer research. Their abnormal expression in many cancer cells modifies the expression of tumour suppressor genes (TSG) and genes involved in normal cellular functions. Indeed, the treatment of cancer cells with HDAC inhibitors is an entry point for renormalization of TSG expression, leading to cancer cell apoptosis. Twenty years of synthetic efforts have led to the FDA approval of only 4 new molecules, based on HDAC inhibition, and many clinical trials have been completed or are underway with various epigenetic drug candidates, used alone or in combinations to potentiate the effects of existing drugs.

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