The p110[delta] structure: mechanisms for selectivity and potency of new PI(3)K inhibitors

Upregulation of PI(3)K signaling pathways is implicated in many diseases, and a number of inhibitors are currently in clinical development. The structure of a PI(3)Kδ kinase domain, along with co-complexes with a diverse range of inhibitors, reveals new insights into mechanisms of inhibition and suggests isoform-selective design strategies.