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Small-Molecule Modulators of the NF-kappa B Pathway Newly Identified by a Translocation-Based Cellular Assay

  作者 Xie, YL; Rinderspacher, A; Liu, YD; Gong, GL; Smith, DH; Wyler, M; Branden, L; Deng, SX  
  选自 期刊  Current Topics in Medicinal Chemistry;  卷期  2009年9-13;  页码  1172-1180  
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[摘要]Nuclear factor kappa B (NF-kappa B) is an important transcription factor. Aberrant regulation of the NF-kappa B pathway is frequently observed in a number of major ailments such as cancer and inflammatory diseases. Hence NF-kappa B modulators have been intensely pursued for their potential therapeutic applications. Numerous reviews have described recent progress in the development of these agents. More recently, a variety of structurally and functionally novel small molecules, identified through high-throughput screens conducted within the Molecular Libraries Screening Center Network (MLSCN) of the NIH Roadmap for Medical Research, have been added to the current list of NF-kappa B regulators. This review will discuss the inhibitors and activators newly discovered by Columbia's Molecular Libraries Screening Center (MLSC) using a well-designed and stable cellular assay.

 
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