Small-molecule modulators of the NF-kappaB pathway newly identified by a translocation-based cellular assay.
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.
Xie
Yuli
Y
Department of Medicine, Columbia University, 630 W 168th Street, New York, NY 10032, USA.
Rinderspacher
Alison
A
Liu
Yidong
Y
Gong
Gangli
G
Smith
Deborah H
DH
Wyler
Michael
M
Brandén
Lars
L
Deng
Shi-Xian
SX
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
D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D016328:NF-kappa B