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A conserved water-mediated hydrogen bond network defines bosutinib’s kinase selectivity
Humans Water Quinolines Nitriles Aniline Compounds src-Family Kinases Amino Acid Substitution Conserved Sequence Substrate Specificity Hydrogen Bonding
2016/5/25
Kinase inhibitors are important cancer drugs, but they tend to display limited target specificity, and their target profiles are often challenging to rationalize in terms of molecular mechanism. Here ...
Structural and Spectroscopic Analysis of the Kinase Inhibitor Bosutinib and an Isomer of Bosutinib Binding to the Abl Tyrosine Kinase Domain
Humans Escherichia coli Benzamides Quinolines Nitriles Aniline Compounds Piperazines Pyrimidines Thiazoles Recombinant Proteins
2016/5/25
Chronic myeloid leukemia (CML) is caused by the kinase activity of the BCR-Abl fusion protein. The Abl inhibitors imatinib, nilotinib and dasatinib are currently used to treat CML, but resistance to t...
THE INHIBITOR-OF-APOPTOSIS PROTEIN SURVIVIN INCREASES P34CDC2 PHOSPHORYLATION AND ENHANCES CELL SURVIVAL AND PROLIFERATION BY PROTECTING THE WEE1 KINASE FROM DEGRADATION BY CASPASE-3
p34Cdc2 Survivin Wee1 Caspase-3 Apoptosis
2015/5/21
The anti-apoptotic protein Survivin and the cyclin-dependent kinase p34Cdc2 are involved in cell cycle progression and apoptosis. Activation of Cdc2 is required for its pro-apoptotic activity, which c...