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Cancer drug development has moved from conventional cytotoxic chemotherapeutics to a more mechanism-based targeted approach towards the common goal of tumour growth arrest. The rapid progress in chromatin research has supplied a plethora of potential targets for intervention in cancer. Here, we focus on the histone deacetylase (HDAC) inhibitors, together with their current status of clinical development and potential utility in cancer therapy. HDACs have been widely implicated in growth and transcriptional control, and inhibition of HDAC activity using small molecules causes apoptosis in tumour cells. We discuss the rationale for the development of HDAC inhibitors as novel anti-cancer agents, the potential clinical application and explore ideas on how we may move towards patient stratification with the possibility of increasing efficacy in the clinic.

Original publication




Journal article


Biochem Pharmacol

Publication Date





1139 - 1144


Acetylation, Animals, Antineoplastic Agents, Cell Cycle, Drug Design, Enzyme Inhibitors, Histone Deacetylase Inhibitors, Histone Deacetylases, Humans, Neoplasms