Epigenetic drug development has quickly gained widespread interest due to the apparent therapeutic efficacy now being demonstrated in preclinical and clinical studies. Drugging the histone methylome remains at the center of discovery with new findings of somatic mutations and deregulation of genes coding for Histone Methyltransferase and Demethylase enzymes. This, in combination with the chemically tractable nature of these enzymes, is providing a strong impetus for therapeutic intervention via pharmacological modulation. Notably, over the past year a rapid expansion of novel demethylase targets, particularly in the Jumonji C domain-containing demethylase family, has substantially deepened the possibilities of regulating chromatin environments via histone methylation. Histone demethylases are now joining the more-established histone methyltransferase targets for clinical development.
As the suite of inhibitors targeting methylation-controlling enzymes expands, challenges can be seen in designing new compounds with higher affinity and specificity; elucidating mechanisms of action of these drugs to shed light on target function in disease; and an overall rigorous approach to target validation in preclinical studies to assess efficacy and toxicity. Cambridge Healthtech Institute will once again convene leaders in epigenetic drug development to provide updates on preclinical and clinical programs, introduce novel targets and chemical matter, and discuss strategies for targeting and validating histone methyltransferases and demethylases.
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Help us cover the Discovery On Target – Histone Methyltransferase and Demethylase meeting, and we’ll set you up with a complimentary registration. You just need to be able to attend the talks and write up a short report for our site. Contact us right away if you’d like to get involved.