Pascal Furet

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: NVP-AEW541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application and abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-ir autophosphorylation.

TL;DR: In vivo evaluation of compound 1h showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3 and support the potential therapeutic use of 1h as a new anticancer agent.

TL;DR: Based upon its clear association with disease, the Bcr-Abl tyrosine kinase in CML represents the ideal target to validate the clinical utility of protein kinase inhibitors as therapeutic agents.

TL;DR: Successful application of a pharmacophore model of the ATP-binding site of the epidermal growth factor receptor (EGFR) kinase led to the identification and optimization of phenylamino-pyrazolo[4,3-d]pyrimidines and substituted isoflavones and quinolones, other classes of potent, selective, and ATP competitive EGFR kinase inhibitors with IC50 values in the low nanomolar range.