Chemical Complementation Assay for MKP-3 (RMI)

MKP-3 (RMI) 的化学互补测定

• 批准号: 7057143
• 负责人: JOHN S. LAZO
• 金额: $ 0.45万
• 依托单位: UNIVERSITY OF PITTSBURGH AT PITTSBURGH
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-09-15 至 2006-09-14
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7057143
• 关键词: biological signal transduction; chemical registry /resource; high throughput technology; mitogen activated protein kinase; phosphatase inhibitor; phosphorylation; reagent /indicator; transfection /expression vector

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.

描述（由申请人提供）：有丝分裂原激活的蛋白激酶磷酸酶-3（MKP-3）是一种双重特异性磷酸酶，具有通过控制有丝分裂原活化蛋白激酶的磷酸化状态来调节细胞内信号转导的中心作用。有大量证据表明MKP-3可能是几种人类疾病的潜在分子靶标。但是，尚未鉴定出该蛋白质磷酸酶的有效或选择性的小分子抑制剂。基于细胞的化学互补分析为筛选该蛋白磷酸酶的细胞活性抑制剂提供了一种新颖的平台技术。该提案将提供足够的试剂，包括细胞和DMA转染载体，以允许高吞吐量筛选100,000种化合物。