Chemical Complementation Assay for MKP-3 (RMI)

说明书(申请人提供)：丝裂原活化蛋白激酶磷酸酶-3(MKP-3)是一种双特异性磷酸酶，通过控制丝裂原活化蛋白激酶的磷酸化状态来调节细胞内的信号转导。有相当多的证据表明，MKP-3可能是几种人类疾病的潜在分子靶点。尽管如此，目前还没有发现这种蛋白磷酸酶的有效或选择性小分子抑制剂。基于细胞的化学互补分析为筛选这种蛋白磷酸酶的细胞活性抑制剂提供了一种新的平台技术。这一建议将提供足够的试剂，包括细胞和DMA转染载体，以允许高通量筛选100,000个化合物。

DESCRIPTION (provided by applicant): Mitogen activated protein kinase phosphatase-3 (MKP-3) is a dual specificity phosphatase that has a central role regulating intracellular signal transduction by controlling the phosphorylation status of mitogen activated protein kinases. There is considerable evidence indicating MKP-3 could be a potential molecular target for several human diseases. Nonetheless, no potent or selective small molecule inhibitors of this protein phosphatase have been identified. Cell-based chemical complementation assays provide a novel platform technology to screen for cell-active inhibitors of this protein phosphatase. This proposal will provide sufficient reagents, including cells and DMA transfection vectors, to permit the high throughput screening of 100,000 compounds.