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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|Titolo:||Inhibition of Bcr-Abl phosphorylation and induction of apoptosis by pyrazolo[3,4-d] pyrimidines in human leukemia cells|
|Citazione:||Manetti, F., Pucci, A., Magnani, M., LOCATELLI G., A., Brullo, C., Naldini, A., et al. (2007). Inhibition of Bcr-Abl phosphorylation and induction of apoptosis by pyrazolo[3,4-d] pyrimidines in human leukemia cells. CHEMMEDCHEM, 2(3), 343-353.|
|Appare nelle tipologie:||1.1 Articolo in rivista|