C-Src and Bcr-Abl are two cytoplasmatic tyrosine kinases (TKs) involved in the development of malignancies. In particular, Bcr-Abl is the etiol. agent of chronic myeloid leukemia, where Src is also involved; the latter is hyperactivated in several solid tumors. Because of the structural homol. between Src and Abl, several compds. 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 pathol. In recent years, the development of such compds. has been promoted by both excellent preclin. and clin. 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 clin. trials and includes information regarding compds. that have appeared in the literature in recent years.

An update on dual Src/Abl inhibitors

MUSUMECI, FRANCESCA;SCHENONE, SILVIA;BRULLO, CHIARA;
2012-01-01

Abstract

C-Src and Bcr-Abl are two cytoplasmatic tyrosine kinases (TKs) involved in the development of malignancies. In particular, Bcr-Abl is the etiol. agent of chronic myeloid leukemia, where Src is also involved; the latter is hyperactivated in several solid tumors. Because of the structural homol. between Src and Abl, several compds. 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 pathol. In recent years, the development of such compds. has been promoted by both excellent preclin. and clin. 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 clin. trials and includes information regarding compds. that have appeared in the literature in recent years.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11567/377038
Citazioni
  • ???jsp.display-item.citation.pmc??? 13
  • Scopus 45
  • ???jsp.display-item.citation.isi??? 43
social impact