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Medical and health sciences
- Morphological sciences
- Oncology
- Morphological sciences
- Oncology
- Morphological sciences
- Oncology
Histone deacetylase (HDAC) inhibitors are a class of compounds that interfere with the function of the histone and non-histone deacetylase enzyme, and blocking of this enzyme results in a variety of biological effects. There are over 18 different HDAC isozymes. Current products on the market (CNS, cancer) are “an-HDAC”inhibitors, blocking diifferent HDAC isozymes simultaneously. This results in limited efficacy and safety issues. Current drug discovery efforts focus on the identification of selective HDAC inhibitors. We have developed a novel class of highly selective and potent HDAC6 inhibitors compared to the current gold standard (tubastatin A). Preliminary biologic testing of a first chemical series revealed 4 compounds to have anti-cancer and anti-invasive activity. A second series is under development to cover surrounding chemical space (available July 2014). The goal of this project is to derive a package of data on two novel chemical series based on tubastatin A that are suitable for consideration by a partner for licensing. It is our ambition to generate data that addresses the requirements of a potential partner.