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Inhibition of Bcr-Abl Phosphorylation and Induction of Apoptosis by Pyrazolo[3,4-d]pyrimidines in Human Leukemia Cells

✍ Scribed by Fabrizio Manetti; Annalisa Pucci; Matteo Magnani; Giada A. Locatelli; Chiara Brullo; Antonella Naldini; Silvia Schenone; Giovanni Maga; Fabio Carraro; Maurizio Botta

Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
460 KB
Volume
2
Category
Article
ISSN
1860-7179

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✦ Synopsis

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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