Dirk Erdmann

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 complex of Grb2-SH2 a BCR-Abl target peptide reveals that the peptide binds in a β-turn conformation; Trp 121 closes the binding site C-terminal to the phosphotyrosyl residue of the ligand and prevents it from assuming the expected extended conformation.

TL;DR: Hsp90 inhibition in B cell acute lymphoblastic leukemia overcomes resistance to JAK2 inhibitors and induces apoptotic cell death in mice treated with these inhibitors.

TL;DR: A novel substituted quinoxaline, NVP-BSK805, which acts in an ATP-competitive manner and displays more than 20-fold selectivity towards JAK2 in vitro, as well as excellent selectivity in broader kinase profiling, is reported.

TL;DR: The results suggest that proteasome inhibition leads to upregulation of specific members of transcription factor families controlling cellular stress response and proliferation.