Probing the mechanism of novel drugs targeted to mitosis in pre-clinical studies


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Robert Wilkinson

Astra Zeneca, UK

Abstract

The Aurora kinases (AK) play a critical role in mitosis and have been suggested as promising targets for cancer therapy due to their frequent overexpression in a variety of tumours (Cheung et al. Expert Opin. Investig. Drugs 2009). Several AK inhibitors are advancing in various stages of development including AZD1152, a selective Aurora B kinase inhibitor (Mortlock et al. J Med Chem. 2007). AZD1152-hydroxy quinazoline pyrazol anilide [hQPA], the active form lacking the phosphate ester, has a novel antitumour mechanism of action in vitro and in vivo,