Receptor tyrosine kinases have been shown to be major pharmaceutical targets involved in disease states such as diabetes and cancer. Target driven therapeutics like small molecules or monoclonal antibodies are already in clinical use and have tremendous influence on new cancer therapies. In most cases either ligand binding to the extracellular domain followed by receptor dimerization or ATP binding to the intracellular kinase domain is inhibited. However, it is still challenging to gain specificity of those inhibitors for certain receptor tyrosine kinase targets. Bead-based assay technologies, such as the xMAP® platform, are ideal tools for the multiplex analysis of 5-20 proteins. Low sample volumes, simple assay protocols, flexibility and robustness are characteristics of bead-based assays that make them well suited for the immunological detection of bio marker and cell signaling proteins. In this presentation we will show results for the simultaneous detection of the ten most relevant receptor tyrosine kinases. The expression profile of more than 50 cell lines as well as breast tumor samples were evaluated with this powerful multiplex tool in a very robust and convenient way. Inhibitor profiling of small molecules under physiological conditions on ten receptor tyrosine kinases will be demonstrated by the detection of their phospho-Tyrosine level. These specificity profiles will help to improve the drug development process and to obtain potentially better drugs in future. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr LB-227.
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