Recent developments in ITC instrumentation, namely MicroCal™ iTC 200 and MicroCal™ Auto iTC 200 have led to an increase in the throughput and decrease in the protein consumption of the technique. In addition, there have been recent methodological advancements that have extended the affinity range that ITC can measure into the mM range. The combination of all these factors has made the technique ideal for fragment-based drug discovery campaigns (FBDD).
This work outlines the role of MicroCal ™Auto iTC 200, in a fragment-based drug discovery program of Sprint Bioscience, to identify and optimize potential drug candidates that will inhibit the activity of Vps34. This class 3 phosphatidylinositol 3 kinase is central to autophagy and has been shown to play an important role in resistance to cancer drugs. As such it has been identified as a target for therapeutic intervention.