In the past few years, there has been an exponential increase in understanding how epigenetic mechanisms control gene expression and cell/tissue functions. The initial interest was in developing therapies targeting epigenetic modifiers focused on oncology where Ezh2 inhibitors showed promise in clinical trial. Epigenetic target classes include methyltransferases, histone deacetylases (HDACs), histone methylases and demethylases, and bromodomain inhibitors. Increasingly, targeting epigenetic gene expression is becoming an area of research in therapeutic areas outside of oncology such as Alzheimer’s disease.

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Our scientists have broad experience working on all classes of epigenetic targets, including bromodomains, methyltransferases and demethylases, ubiquitin ligases and deubiquitinases, and histone deacetylases, encompassing target discovery, assay development and screening, in silico library design, and medicinal chemistry. We are proud to have contributed to the discovery of belinostat, an approved drug for refractory peripheral T-cell lymphoma that is a histone deacetylase inhibitor.

  • Potent, Selective, and CNS-​Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors. ACS Med. Chem. Lett. 2016, 1, 34-39. Abstract.
  • The Pan-HDAC Inhibitor Panobinostat Acts as a Sensitizer for Erlotinib Activity in EGFR-Mutated and -Wildtype Non-Small Cell Lung Cancer Cells. BMC Cancer. 2015, 15, 947. Full Text.
  • The Making of an HDAC Inhibitor. Eureka. January 2015. Full Text.
  • Getting to the Crux of Epigenetic Targets – Effective Drug Discovery Necessitates New Tools and Technologies That Can Get the Job Done. Genetic Engineering News. July 2012. Full Text.
  • Epigenetics – The Social Network of Our Genes. Nature Reviews Drug Discovery. March 2011. Volume 10, Number 3. Full Text.