Target: PI3K- p110β/δ
The phosphoinositide 3-kinases (PI3Ks) constitute a family of lipid kinase enzymes which – through signal transduction pathway control, emerging functions in the tumor microenvironment, and mutational status – have become key targets for cancer therapy. Our clinical program focuses on isoforms PI3K-β and PI3K-δ.
Wild-type PI3K-β is oncogenic when over-expressed, and, notably, can drive the growth of tumors that are defective in PTEN, the negative-regulator phosphatase of PI3K signaling. A role for PI3K-β in tumor metastasis has emerged, and rare mutations of the enzyme have been reported in cancer.
PI3K-δ is primarily expressed in the hematopoietic system and it plays a critical role in the signaling of hematological cancers. A role for PI3K-δ in regulatory T-cell (Treg) activity has also been discovered, with inhibition resulting in CTL activation and primary solid tumor growth inhibition.