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

Autor: Xie, Yuli, Rinderspacher, Alison, Liu, Yidong, Gong, Gangli, Smith, Deborah, Wyler, Michael, Branden, Lars, Deng, Shi-Xian
Zdroj: Current Topics in Medicinal Chemistry; September 2009, Vol. 9 Issue: 13 p1172-1180, 9p
Abstrakt: Nuclear factor kappa B (NF-B) is an important transcription factor. Aberrant regulation of the NF-B pathway is frequently observed in a number of major ailments such as cancer and inflammatory diseases. Hence NF-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-B regulators. This review will discuss the inhibitors and activators newly discovered by Columbias Molecular Libraries Screening Center (MLSC) using a well-designed and stable cellular assay.
Databáze: Supplemental Index