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Updated: May 22, 2026

Genome-wide Mapping of Drug-DNA Interactions in Cells with COSMIC (Crosslinking of Small Molecules to Isolate Chromatin)
Published on: January 20, 2016
DNA-binding small molecules as inhibitors of transcription factors
Chung-Hang Leung1, Daniel Shiu-Hin Chan, Victor Pui-Yan Ma
1Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China. duncanleung@umac.mo
Abstract:
Accumulating evidence implicating the role of aberrant transcription factor signaling in the pathogenesis of various human diseases such as cancer and inflammation has stimulated the development of small molecule ligands capable of targeting transcription factor activity and modulating gene expression. The use of DNA-binding small molecules to selectively inhibit transcription factor-DNA interactions represents one possible approach toward this goal. In this review, we summarize the development of DNA-binding small molecule inhibitors of transcription factors from 2004 to 2011, and their binding mode and therapeutic potential will be discussed.
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