Giorgio Caravatti

TL;DR: An association between PKC inhibition and anti‐proliferative and anti-tumor activity is suggested and staurosporine and CGP 41 251 exerted growth inhibition in the human bladder carcinoma line T‐24, human promyelocytic leukemia line HL‐60 and bovine corneal endothelial cells at concentrations which correlated well with in vitroPKC inhibition.

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: 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: Data indicate that AEE788 has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters, and is currently in Phase I clinical trials in oncology.

TL;DR: Three successful examples of drug design at Novartis using a tyrosine kinase as a molecular target are described and promising data from phase I and II clinical trials in CML patients support the fact that the STI571 represents a new treatment modality for CML.