Abstract: |
Overexpression of the transmembrane tyrosine kinases Her2 and EGFR is associated with aggressive malignancies, and several therapeutic strategies targeting the two receptors are now in various stages of clinical development. Most of the known agents block the activation or inhibit the activity of the kinases; however, a more significant therapeutic outcome may result from degrading these oncoproteins. Here, we report the development of a microtiter cell-based assay that sensitively detects cellular levels of Her2 and EGFR. The assay is useful in identifying small molecules that alter cellular levels of these kinases and in quantifying their effect. The method gives results comparable to Western blot, but it is faster, less labor intensive, and amenable to high throughput. |
Keywords: |
genetics; reproducibility; reproducibility of results; metabolism; actin; cells, cultured; proto oncogene; epidermal growth factor receptor; neoplasm proteins; receptor, epidermal growth factor; enzymology; gene library; cell line, tumor; breast neoplasms; blotting, western; biosynthesis; statistical analysis; data interpretation, statistical; cell culture; breast tumor; bioassay; tumor protein; tumor cell line; western blotting; cell count; biological assay; actins; genes, erbb-2; humans; human; female; article
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