Project

Opportunity to develop novel HDAC6 inhibitors for therapeutic use

Acronym
HDAC6 inhibitors
Duration
15 August 2014 → 15 August 2017
Funding
Regional and community funding: Industrial Research Fund
Research disciplines
  • Medical and health sciences
    • Morphological sciences
    • Oncology
    • Morphological sciences
    • Oncology
    • Morphological sciences
    • Oncology
Keywords
immunology cancer HDAC6 inhibitors HDAC validation drug discovery
 
Project description

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.