Abstract 362: TR-FRET binding assays for PI3K family inhibitors
| Autor: | Jill K. Wolken, Steven M. Riddle, Sara B. Hereley, Hildegard C. Eliason, William J. Frazee |
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| Rok vydání: | 2010 |
| Předmět: | |
| Zdroj: | Cancer Research. 70:362-362 |
| ISSN: | 1538-7445 0008-5472 |
| DOI: | 10.1158/1538-7445.am10-362 |
| Popis: | There is a great clinical need to develop selective, high affinity kinase inhibitors. While many high throughput kinase activity assays have become readily available, easy-to-use and cost-effective, activity-based assays have significant limitations in terms of both the extent of target coverage and the type of information they can provide about compounds. We have developed a competitive TR-FRET binding assay platform for characterization of protein kinase inhibitors. This assay platform has several advantages over traditional activity-based assays, in part due to simplicity of the assays as well as the ability to measure binding events in real time. To extend the breadth of target coverage of this platform, we have developed novel tracers for Class I PI3-kinases and the related protein kinase mTOR. We present a comparison of inhibitor potencies measured in binding assays relative to kinase activity assays for a diverse set of commonly used PI3 kinase family inhibitors. These novel assays enable simple, rapid measurements of IC50 values for PI3 kinases and mTOR. 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 362. |
| Databáze: | OpenAIRE |
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