Discussion

As the understanding of the field of epigenetics is increasing at a rapid pace, drug discovery companies are developing the molecular tools and future drugs addressing this group of targets. Histone lysine demethylases (KDMs) is an interesting subclass of epigenetic enzymes, with relevance for oncological, neurological and anti-viral indications. This talk will focus on Beactica’s drug discovery programmes with epigenetic targets LSD1/KDM1a and KDM4C/JMJD2C.

Based on Beactica SPR biosensor-based drug discovery platform, small molecular reversible inhibitors have been developed from fragment hits. Several independent series of inhibitors and allosteric modulators have been characterized, utilizing structural biology, a range of biophysical methods and in vitro efficacy assessments. Fragment-based lead generation strategies will be discussed in the small company’s perspective, with the quest to shape the optimal mix of internal resources and CROs with academic collaborations. The talk will span over target identification and validation, screen and hit characterization, lead generation through target engagement, in vitro efficacy and ADME, to clinical strategies directing lead optimization efforts.