DNA-Binding Small Molecules as Inhibitors of Transcription Factors

Chung Hang Leung*, Daniel Shiu Hin Chan, Victor Pui Yan Ma, Edmond Dik Lung MA

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

46 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)823-846
Number of pages24
JournalMedicinal Research Reviews
Issue number4
Publication statusPublished - Jul 2013

Scopus Subject Areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

User-Defined Keywords

  • Groove binding
  • Inhibitor
  • Intercalation
  • Small molecule
  • Transcription factor


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