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Specific Inhibition of Formation of Transcription Complexes by a Calicheamicin Oligosaccharide: A Paradigm for the Development of Transcriptional Antagonists

Steffan N. Ho, Serge H. Boyer, Stuart L. Schreiber, Samuel J. Danishefsky and Gerald R. Crabtree
Proceedings of the National Academy of Sciences of the United States of America
Vol. 91, No. 20 (Sep. 27, 1994), pp. 9203-9207
Stable URL: http://www.jstor.org/stable/2365804
Page Count: 5
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Since scans are not currently available to screen readers, please contact JSTOR User Support for access. We'll provide a PDF copy for your screen reader.
Specific Inhibition of Formation of Transcription Complexes by a Calicheamicin Oligosaccharide: A Paradigm for the Development of Transcriptional Antagonists
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Abstract

Sequence-specific DNA ligands that antagonize DNA-protein interactions represent a potentially powerful means of modulating gene expression. Calicheamicin γ1 I, a member of the DNA-cleaving enediyne class of anticancer antibiotics, binds to specific DNA sequences through an aryltetrasaccharide domain. To take advantage of this unique sequence-specific recognition capability, the methyl glycoside of the aryltetrasaccharide of calicheamicin γI 1 (CLM-MG) was used to investigate the ability of glycoconjugate DNA ligands to inhibit DNA-protein interactions. CLM-MG inhibits the formation of DNA-protein complexes at micromolar concentrations in a sequence-specific manner and rapidly dissociates preformed complexes. CLM-MG also inhibits transcription in vivo with similar sequence specificity. These results suggest a strategy for the development of a class of novel biological probes and therapeutic agents.

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