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Sequence-specific trapping of topoisomerase I by DNA binding polyamide-camptothecin conjugates

Wang, Clay C. C. and Dervan, Peter B. (2001) Sequence-specific trapping of topoisomerase I by DNA binding polyamide-camptothecin conjugates. Journal of the American Chemical Society, 123 (36). pp. 8657-8661. ISSN 0002-7863. doi:10.1021/ja010392p.

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Hairpin pyrrole−imidazole polyamides are synthetic ligands that bind in the minor groove of DNA with affinities and specificities comparable to those of DNA binding proteins. Three polyamide−camptothecin conjugates 1−3 with linkers varying in length between 7, 13, and 18 atoms were synthesized to trap the enzyme Topoisomerase I and induce cleavage at predetermined DNA sites. One of these, polyamide−camptothecin conjugate 3 at nanomolar concentration (50 nM) in the presence of Topo I (37 °C), induces DNA cleavage between three and four base pairs from the polyamide binding site in high yield (77%).

Item Type:Article
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URLURL TypeDescription Information
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2001 American Chemical Society. Received February 13, 2001; Publication Date (Web): August 16, 2001. We are grateful to the National Institutes of Health (GM-27681) for research support and a traineeship award (GM-08501) to C.C.C.W.
Funding AgencyGrant Number
NIH Predoctoral FellowshipGM-08501
Issue or Number:36
Record Number:CaltechAUTHORS:20160510-082725087
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Official Citation:Sequence-Specific Trapping of Topoisomerase I by DNA Binding Polyamide−Camptothecin Conjugates Clay C. C. Wang and Peter B. Dervan Journal of the American Chemical Society 2001 123 (36), 8657-8661 DOI: 10.1021/ja010392p
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66821
Deposited By: Victoria Brennan
Deposited On:18 May 2016 19:00
Last Modified:11 Nov 2021 00:03

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