Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5294
Title: Inhibition of Bcr-Abl phosphorylation and induction of apoptosis by pyrazolo[3,4-d] pyrimidines in human leukemia cells
Authors: Manetti, Fabrizio 
Pucci, Annalisa
Magnani, M
LOCATELLI G., A
Brullo, C
Naldini, Antonella
Schenone, S
Maga, G
Carraro, Fabio
Botta, Maurizio 
Keywords: Antineoplastic Agents; Enzyme Inhibitors; Proto-Oncogene Proteins pp60(c-src)-EC 2.7.1.112; 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.
Description: 
36097
URI: http://hdl.handle.net/20.500.12779/5294
ISSN: 1860-7179
DOI: 10.1002/cmdc.200600214
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