The cytoplasmatic tyrosine in kinase c-Src is involved in the regulation of several cell functions including adhesion, invasion, proliferation, survival and angiogenesis. Src activity is strictly regulated in healthy cells, whereas its overexpression or hyperactivation plays a crit. role during tumor development. Recently it has been suggested that the oncogenic potential of Src is linked to its role in the activation of key signalling mols. involved in several cell pathways, rather than its direct activity. For all these reasons Src represents a promising therapeutic target for the treatment of tumors. In this article a no. of examples of c-Src inhibitors appeared in selected patents from 2006 to early 2011 will be reported, focusing on their chem. features and, whenever possible, on structure-activity relationships and mechanism of action. Examples of type I or II ATP-competitive inhibitors or substrate competitive inhibitors will be presented. The research in this field is very active and will probably lead to the discovery of therapeutically useful compds., both c-Src selective and multitargeted inhibitors, that acting on different cell pathways could be more effective in blocking cancer development. However, only the results of clin. trials will show in the near future the most promising compds.

Src kinase inhibitors: an update on patented compounds

SCHENONE, SILVIA;BRULLO, CHIARA;MUSUMECI, FRANCESCA;
2011-01-01

Abstract

The cytoplasmatic tyrosine in kinase c-Src is involved in the regulation of several cell functions including adhesion, invasion, proliferation, survival and angiogenesis. Src activity is strictly regulated in healthy cells, whereas its overexpression or hyperactivation plays a crit. role during tumor development. Recently it has been suggested that the oncogenic potential of Src is linked to its role in the activation of key signalling mols. involved in several cell pathways, rather than its direct activity. For all these reasons Src represents a promising therapeutic target for the treatment of tumors. In this article a no. of examples of c-Src inhibitors appeared in selected patents from 2006 to early 2011 will be reported, focusing on their chem. features and, whenever possible, on structure-activity relationships and mechanism of action. Examples of type I or II ATP-competitive inhibitors or substrate competitive inhibitors will be presented. The research in this field is very active and will probably lead to the discovery of therapeutically useful compds., both c-Src selective and multitargeted inhibitors, that acting on different cell pathways could be more effective in blocking cancer development. However, only the results of clin. trials will show in the near future the most promising compds.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11567/296900
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