title: DNA-binding small molecules as inhibitors of transcription factors.
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.
authors.affiliation: Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China. duncanleung@umac.mo
authors.forename: Chung-Hang
authors.initials: CH
authors.lastname: Leung
authors.forename: Daniel Shiu-Hin
authors.initials: DS
authors.lastname: Chan
authors.forename: Victor Pui-Yan
authors.initials: VP
authors.lastname: Ma
authors.forename: Dik-Lung
authors.initials: DL
authors.lastname: Ma
mesh_terms: D000818:Animals; D004247:DNA / Q000378:metabolism*; D005057:Eukaryotic Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D011485:Protein Binding / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D014157:Transcription Factors / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D061785:Transcription Initiation, Genetic / Q000187:drug effects
chemical_list: D054852:Small Molecule Libraries; D014157:Transcription Factors; D004247:DNA