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Cellular Targets of Gefitinib

¹ Axxima Pharmaceuticals AG, Munich, Germany and ² Vichem Chemie Ltd. and ³ Department of Medicinal Chemistry, Peptide Biochemistry Research Group, Semmelweis University, Budapest, Hungary

Requests for reprints: Henrik Daub, Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, Munich, Germany. Phone:49-89-550-65-356. E-mail: henrik.daub{at}axxima.com.

Targeted inhibition of protein kinases with small molecule drugs has evolved into a viable approach for anticancer therapy. However, the true selectivity of these therapeutic agents has remained unclear. Here, we used a proteomic method to profile the cellular targets of the clinical epidermal growth factor receptor kinase inhibitor gefitinib. Our data suggest alternative cellular modes of action for gefitinib and provide rationales for the development of related drugs.

Key Words: gefitinib • selectivity • proteomics • protein kinases • drug development

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