Presentation: 1B03

Although kinases and phosphatases are prominent drug targets, only a small number has been associated with particular diseases and therefore been addressed by drug development. The majority of kinases and phosphatases has not been characterized yet. However, the availability of RNA interference for efficient and reproducible silencing of individual genes in human cells now provides the opportunity to gain functional information on each individual target. We applied kinase and phosphatase siRNA libraries to multi-parametric high-content assays using the automated high-throughput microscope OPERA. First, we characterized the libraries in a time-course for the impact of target mRNA down-regulation on cell viability and apoptosis to define a screening window. Subsequently, the libraries were applied in primary screens for viral infection; in secondary assays the pathways were dissected to characterize novel targets in regulating endocytosis. The complex phenotypic patterns were compared with those of natural phosphatase inhibitors and their derivates.

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