Recent discovery of phosphoinositide 3-kinase γ inhibitors for the treatment of immune diseases and cancers.

Recently, PI3Kγ, a vital kinase, which involved in numerous intracellular signaling pathways, has been considered as a promising drug target for the treatment of immune diseases and certain cancers. Before the 21st century, few selective PI3Kγ inhibitors were discovered because no non-conserved structure in the ATP binding sites of PI3Kγ had been found. Since the discovery of the non-ATP binding pocket, the reported structures of potent and selective PI3Kγ inhibitors have become more diverse, and one compound (IPI549) has entered Phase I clinical trial. This review centers on a general overview of PI3Kγ inhibitors in clinical and preclinical as well as further therapeutic applications in human diseases.