Discovery of inhibitors of aberrant gene transcription from libraries of DNA binding molecules: Inhibition of LEF-1-mediated gene transcription and oncogenic …

JS Stover, J Shi, W Jin, PK Vogt…

文献索引：Stover, James S.; Shi, Jin; Jin, Wei; Vogt, Peter K.; Boger, Dale L. Journal of the American Chemical Society, 2009 , vol. 131, p. 3342 - 3348

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被引用次数: 34

摘要

The screening of a> 9000 compound library of synthetic DNA binding molecules for selective binding to the consensus sequence of the transcription factor LEF-1 followed by assessment of the candidate compounds in a series of assays that characterized functional activity (disruption of DNA− LEF-1 binding) at the intended target and site (inhibition of intracellular LEF-1-mediated gene transcription) resulting in a desired phenotypic cellular ...