Discovery of a Potent, Selective, Bio-Available & Highly Efficacious DNAPK Inhibitor

Time: 1:00 pm
day: Day Two


• The lecture will introduce the importance of DNA-dependent protein kinase (DNA-PK), a serine-threonine protein kinase, in repairing double-strand DNA breaks and in the DNA damage response
• We have optimized an initial lead series to identify a potent and selective DNA-PK inhibitor. An overview of the optimization strategy will be presented, along with the key lessons learned during this discovery process
• The lead molecule’s in vitro, and cross-species PK profile will be presented, demonstrating the excellent profile of the lead DNA-PK inhibitor.
• The efficacy of the lead DNA-PK inhibitor in a mouse FaDu thigh muscle xenograft model, in combination with ionizing radiation treatment, will be presented