title: Small-molecule modulators of the NF-kappaB pathway newly identified by a translocation-based cellular assay.
abstract: Nuclear factor kappa B (NF-kappaB) is an important transcription factor. Aberrant regulation of the NF-kappaB pathway is frequently observed in a number of major ailments such as cancer and inflammatory diseases. Hence NF-kappaB 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-kappaB 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.
authors.affiliation: Department of Medicine, Columbia University, 630 W 168th Street, New York, NY 10032, USA.
authors.forename: Yuli
authors.initials: Y
authors.lastname: Xie
authors.forename: Alison
authors.initials: A
authors.lastname: Rinderspacher
authors.forename: Yidong
authors.initials: Y
authors.lastname: Liu
authors.forename: Gangli
authors.initials: G
authors.lastname: Gong
authors.forename: Deborah H
authors.initials: DH
authors.lastname: Smith
authors.forename: Michael
authors.initials: M
authors.lastname: Wyler
authors.forename: Lars
authors.initials: L
authors.lastname: Brandén
authors.forename: Shi-Xian
authors.initials: SX
authors.lastname: Deng
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001681:Biological Assay / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D006801:Humans; D008970:Molecular Weight; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D016328:NF-kappa B