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De-mystifying the Epigenetic Free for All: Pharmacophore Modeling for Epigenetic Cancer Therapy

Viviane Rösner de Almeida, Algemir Lunardi Brunetto, Gilberto Schwartsmann, Rafael Roesler and Ana Lucia Abujamra

Epigenetic regulators have quickly become one of the most widely studied therapeutic agents for a vast array of diseases, making histone deacetylase inhibitors (HDIs) and DNA methyl-transferase (DNMT) inhibitors commonly used molecules in pre-clinical and clinical anti-cancer studies. Their ability to regulate gene expression and to potentiate the effects of other chemotherapeutic drugs has put HDIs and DNMT inhibitors in the spotlight not only as single agents, but also as combined therapy. The plethora of HDIs and DNMT inhibitors available nowadays has led to promising results in Phase I, II and III clinical oncology studies. While it was first believed that these molecules would all have an additive or synergistic effect when combined with the classical chemotherapeutic drugs available, our group and others have shown that epigenetic regulators potentiate the effects of some, but not all, anti-cancer molecules. Pharmacophore modeling may therefore serve the purpose to optimize pre-clinical research and to develop more efficient and targeted therapies incorporating epigenetic regulators.