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PI3Kα/mTOR inhibitors for the treatment of cancer

The PI3Kα/Akt/mTOR signaling pathway is considered a central link in cell signaling as it receives growth signals and propagates them through a series of phosphorylations and dephosphorylations of downstream effectors. Normally, this pathway is essential for vital cellular processes such as cell growth, metabolism and survival.  Dysregulation of the PI3Kα/Akt/mTOR signaling pathway, however, has been confirmed in many different types of human tumors such as gastrointestinal, breast, ovarian, prostate and glioblastoma. Targeting any single mechanism in this pathway has provided limited success in the treatment of cancer due to rapid resistance and compensatory mechanisms.  This has lead numerous research team to focus on the identification of compounds capable to targeting multiple points in the PI3Kα/Akt/mTOR signaling pathway.  Our efforts have focused on the identification of novel ATP-competitive dual PI3Kα/mTOR inhibitors and has produced a series of compounds with low nanomolar potency at both targets. 

Temple University
Moulder Center for Drug Discovery Research

Temple University School of Pharmacy
3307 N Broad Street
Philadelphia, PA 19140