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  • 标题:Synthesis and screening of small molecule libraries active in binding to DNA
  • 本地全文:下载
  • 作者:Gerald W. Shipps ; Kent E. Pryor ; Jun Xian
  • 期刊名称:Proceedings of the National Academy of Sciences
  • 印刷版ISSN:0027-8424
  • 电子版ISSN:1091-6490
  • 出版年度:1997
  • 卷号:94
  • 期号:22
  • 页码:11833-11838
  • DOI:10.1073/pnas.94.22.11833
  • 语种:English
  • 出版社:The National Academy of Sciences of the United States of America
  • 摘要:Five synthetic combinatorial libraries of 2,080 components each were screened as mixtures for inhibition of DNA binding to two transcription factors. Rapid, solution-phase synthesis coupled to a gel-shift assay led to the identification of two compounds active at a 5- to 10-{micro}M concentration level. The likely mode of inhibition is intercalation between DNA base pairs. The efficient deconvolution through sublibrary synthesis augurs well for the use of large mixtures of small, nonpeptide molecules in biological screens.
  • 关键词:diversity ; combinatorial chemistry ; ureas ; gel-shift assay ; DNA binding
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