Drug-Resistant Phosphatidylinositol 3-Kinase: Guidance for the Preemptive Strike

In this issue of Cancer Cell, Zunder et al. (2008) describe surprising findings from investigating inhibitor-resistant mutations in the affinity pocket of p110α of phosphatidylinositol 3-kinase (PI3K). Information on these critical residues provides a road map for generating novel PI3K inhibitors that can overcome the anticipated resistance mutations.