New Assignments for Multi-tasking Signal Transduction Inhibitors (Relates to Article by Chen, et al. FastForward 25 January 2006).

Posted by rob on March 23, 2006 under Uncategorized | Be the First to Comment

An article presented in this issue of Molecular Pharmacology (p. …) provides an intriguing example of how tyrosine kinase inhibitors can be put to many uses. In this article, the action of dasatinib (BMS-354825) is contrasted to that of imatinib, a kinase inhibitor that is currently being used to treat chronic myelogenous leukemia and other disorders. Both inhibitors target several tyrosine kinases, including Bcr-Abl and the platelet-derived growth factor receptor (PDGFR). Up to this point, the PDGFR has not been a primary therapeutic target for these agents. The work of Chen and colleagues shows that BMS-354825 is a particularly potent inhibitor of PDGFR, and that the compound also targets Src kinase. The authors suggest that this combination of activities could be useful in the treatment of vascular obstructive diseases. While a lack of absolute specificity has classically been regarded as a pharmacologic drawback, this study exemplifies that drugs with multiple molecular targets can potentially provide a very beneficial spectrum of therapeutic activities in multiple disease states.
New Assignments for Multi-tasking Signal Transduction Inhibitors (Relates to Article by Chen, et al. FastForward 25 January 2006).