Isoform Selective PI3K-beta Inhibitors

Although PI3K/AKT has undoubtedly been one of the most important pathways that impact tumorigenesis and proliferation, PI3K‐beta has not been considered as a stand‐alone target for potential cancer treatment until the recent discovery of the key role that PI3K‐beta plays in phosphatase and TENsin homolog (PTEN)‐deficient tumors. Medicinal chemistry efforts from the pharmaceutical industry and academia in the past few years have led to significant advancements in understanding beta isoform selectivity and in the development of a clinical drug candidate.