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|Title:||Inhibition of Bcr-Abl phosphorylation and induction of apoptosis by pyrazolo[3,4-d] pyrimidines in human leukemia cells||Authors:||Manetti, Fabrizio
LOCATELLI G., A
|Keywords:||Antineoplastic Agents; Enzyme Inhibitors; Proto-Oncogene Proteins pp60(c-src)-EC 126.96.36.199; Pyrazoles; Pyrimidines||Issue Date:||2007||Project:||None||Journal:||CHEMMEDCHEM||Abstract:||
A series of pyrazolo[3,4-d]pyrimidines, previously found to be Src inhibitors, was tested for their ability to inhibit proliferation of three Bcr-Abl-positive human leukemia cell lines (K-562, KU-812, and MEG-01), on the basis of the experimental evidence that various Src inhibitors are also active against Bcr-Abl kinase (the so called dual Src/Abl inhibitors). They reduce Bcr-Abl tyrosine phosphorylation and promote apoptosis of the Bcr-Abl-expressing cells. A cell-free enzymatic assay on isolated c-Abl confirmed that such compounds directly inhibit Abl activity. Finally, molecular modeling simulations were also performed to hypothesize the binding mode of the compounds into the Abl binding site.
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