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Novel Small-Molecule Inhibitors of Src Kinase for Cancer Therapy

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Cancer

Part of the book series: Topics in Medicinal Chemistry ((TMC,volume 1))

Abstract

Drug discovery for cancer therapy is making extraordinary progress within the realm of advancing noveloncogenic protein kinase inhibitor lead compounds of varying chemical structure and biological mechanism.About 30 years ago, the first oncogenic protein kinase, pp60src (Src), wasdiscovered and provided a prototype of the now-existing superfamily of Tyr, Ser/Thr and dual-specificityprotein kinases. This review highlights Src kinase with respect to its known genetic and signal transductionpathways. Furthermore, several key Src kinase inhibitors are highlighted with respect to structural biology,drug design, chemical diversity, and biological properties. Noteworthy are a few novel small moleculesthat have enabled preclinical proof-of-concept studies as well as providing promising clinical candidatesfor cancer therapy.

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    Tomi K. Sawyer

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Sawyer, T.K. (2007). Novel Small-Molecule Inhibitors of Src Kinase for Cancer Therapy. In: Bradbury, R.H. (eds) Cancer. Topics in Medicinal Chemistry, vol 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/7355_2006_010

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