Article
Characterization, chemical optimization and anti-tumour activity of a tubulin poison identified by a p53-based phenotypic screen.
Cell cycle (Georgetown, Tex.) - 1 Nov 2008
Staples Oliver D, Hollick Jonathan J, Campbell Johanna, Higgins Maureen, McCarthy Anna R, Appleyard Virginia, Murray Karen E, Baker Lee, Thompson Alastair, Ronseaux Sebastien, Slawin Alexandra M Z, Lane David P, Westwood Nicholas J, Lain Sonia
Abstract excerpt
A robust p53 cell-based assay that exploits p53's function as a transcription factor was used to screen a small molecule library and identify bioactive small molecules with potential antitumor activity. Unexpectedly, the majority of the highest ranking hit compounds from this screen arrest cells in mitosis and most of them impair polymerization of tubulin in cells and in vitro. One of these novel compounds,...
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