Patrick Chène

TL;DR: The preclinical data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties, and the compound was well tolerated, displayed disease stasis when administered orally, and enhanced the efficacy of other anticancer agents when used in in vivo combination studies.

TL;DR: In this study, inhibiting the p53–MDM2 interaction with synthetic molecules should lead to p53-mediated cell-cycle arrest or apoptosis in p 53-positive stressed cells.

TL;DR: The biologic characterization of the 2-morpholino pyrimidine derivative pan-PI3K inhibitor NVP-BKM120 shows dose-dependent in vivo pharmacodynamic activity as measured by significant inhibition of p-Akt and tumor growth inhibition in mechanistic xenograft models and behaves synergistically when combined with either targeted agentssuch as MEK or HER2 inhibitors or with cytotoxic agents such as docetaxel or temozolomide.

TL;DR: The biologic properties of the 2-aminothiazole derivative NVP-BYL719, a selective inhibitor of PI3Kα and its most common oncogenic mutant forms, are reported and it is found that PIK3CA mutation was the foremost positive predictor of sensitivity while revealing additional positive and negative associations such as Pik3CA amplification and PTEN mutation, respectively.

TL;DR: The p53-hdm2 interaction biochemically is characterized and the potential of a series of peptide inhibitors, derived from previously described mdm2 binding peptide display phage, to disrupt this interaction in ELISA assays are analysed.