Department of Chemistry
DNA-binding small molecules as inhibitors of transcription factors
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. © 2012 Wiley Periodicals, Inc.
Groove binding, Inhibitor, Intercalation, Small molecule, Transcription factor
Source Publication Title
Medicinal Research Reviews
Leung, Chung-Hang, Daniel Shiu-Hin Chan, Victor Pui-Yan Ma, and Dik-Lung Ma. "DNA-binding small molecules as inhibitors of transcription factors." Medicinal Research Reviews 33.4 (2013): 823-846.