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An update on dual Src/Abl inhibitors

Authors :
Chiara Brullo
Silvia Schenone
Maurizio Botta
Francesca Musumeci
Source :
Future Medicinal Chemistry. 4:799-822
Publication Year :
2012
Publisher :
Future Science Ltd, 2012.

Abstract

c-Src and Bcr-Abl are two cytoplasmatic tyrosine kinases (TKs) involved in the development of malignancies. In particular, Bcr-Abl is the etiologic agent of chronic myeloid leukemia, where Src is also involved; the latter is hyperactivated in several solid tumors. Because of the structural homology between Src and Abl, several compounds originally synthesized as Src inhibitors have also been shown to be Abl inhibitors, useful in overcoming the onset of some types of chronic myeloid leukemia resistances, which frequently appear in the advanced phases of pathology. In recent years, the development of such compounds has been promoted by both excellent preclinical and clinical results, and by the theory that dual or multi-targeted inhibitors might be more effective than selective inhibitors. This review is an update on the most important dual inhibitors already in clinical trials and includes information regarding compounds that have appeared in the literature in recent years.

Details

ISSN :
17568927 and 17568919
Volume :
4
Database :
OpenAIRE
Journal :
Future Medicinal Chemistry
Accession number :
edsair.doi.dedup.....8883dd8fa7eb6f63231b4b7fe62c46cf
Full Text :
https://doi.org/10.4155/fmc.12.29