Related Experiment Video
Updated: May 23, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Pyrazolopyrimidines as dual Akt/p70S6K inhibitors
Kenneth D Rice1, Moon H Kim, Joerg Bussenius
1Exelixis, 210 E. Grand Avenue, South San Francisco, CA 94080, USA.
Abstract:
Activation of the PI3K/Akt/mTOR kinase pathway is frequently associated with human cancer. Selective inhibition of p70S6Kinase, which is the last kinase in the PI3K pathway, is not sufficient for strong tumor growth inhibition and can lead to activation of upstream proteins including Akt through relief of a negative feedback loop. Targeting multiple sites in the PI3K pathway might be beneficial for optimal activity. In this manuscript we report the design of dual Akt/p70S6K inhibitors and the evaluation of the lead compound 11b in vivo, which was eventually advanced into clinical development.
Related Concept Videos
Inhibitors of Viral Protein Synthesis
PI3K/mTOR/AKT Signaling Pathway
Inhibition of CDK Activity
Inhibition of Cdk Activity
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
