It has been more than 20 years since phosphatidylinositol 3-kinase (PI3K) was first discovered. The transforming ability of viral oncoproteins relied on an association with a PI3K lipid kinase activity. Over the ensuing years, studies established the central role of PI3K signaling in several cellular processes critical for cancer progression, including metabolism, growth, survival, and motility. Inappropriate co-option of PI3K signaling is one of the most frequent occurrences in human cancer. Consequently, significant efforts have been made to generate inhibitors of the PI3K pathway to treat cancers. Loss of PTEN protein results in upregulation of the PI3K/AKT pathway, which appears dependent on the PI3Kβ isoform. Inhibitors of PI3Kβ have potential to reduce growth of tumors in which loss of PTEN drives tumor progression.
Porta C, Paglino C, Mosca A. Targeting PI3K/Akt/mTOR signaling in cancer[J]. Targeting PI3K/mTOR signaling in cancer, 2014: 47.
Courtney K D, Corcoran R B, Engelman J A. The PI3K pathway as drug target in human cancer[J]. Journal of Clinical Oncology, 2010, 28(6): 1075-1083.