Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway

Background: Among promising targeted therapies for cancer treatment, phosphatidylinositol 3-kinase pathway inhibitors have in the last 3 years continued to retain the attention of both academic institutions and pharmaceutical companies. The large amount of published clinical and preclinical data has indeed confirmed the preponderant role of this so-called survival pathway for tumor maintenance. Discussion: Global efforts have, therefore, been deployed that have led to the genesis of a panoply of small molecule inhibitors. This review will focus on updating the reader on the current medicinal chemistry efforts targeting this pathway. Conclusions: Recent discoveries important for patient stratification, quantification of target modulation in humans and combination therapies will be presented and discussed.