[Webinar] How to better optimize an oncology drug discovery program
Register for this webinar discussing how conventional and innovative integrated technological skills should be incorporated into an oncology program.
Read more Authors: Nerina Dodic, Nicolas Ancellin, Anne Bouillot, Nathan Butin, Cedric Charrier, Marie-Hélène Fouchet, Alain Laroze, Anne-Pascale Luzy, Alexandre Moquette, Guillaume Serin, Christophe Parsy
Abstract: With small macrocyclic “probes” from our proprietary library in the low nanomolar range IC50, we turned our attention to CDK9 inhibitors with good selectivity profile against CDK1/2/5/7 as a starting point for building bifunctional small macrocyclic kinase degraders. Although the ATP binding site of the CDKs are structurally similar, developing a small macrocyclic PROTAC degrader could enhanced the selectivity of the parent molecule by preferential ubiquitination of lysine exposed residues among the different CDKs…