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. 2001;40(16):3045-8.
doi: 10.1002/1521-3773(20010817)40:16<3045::AID-ANIE3045>3.0.CO;2-A.

Directing topoisomerase I mediated DNA cleavage to specific sites by camptothecin tethered to minor- and major-groove ligands

P B Arimondo  1 , C Bailly, A S Boutorine, V A Ryabinin, A N Syniakov, J S Sun, T Garestier, C Hélène
Affiliations

Directing topoisomerase I mediated DNA cleavage to specific sites by camptothecin tethered to minor- and major-groove ligands

P B Arimondo et al. Angew Chem Int Ed Engl. 2001.

Abstract

The covalent linkage of a hairpin polyamide, which binds in the minor groove, to camptothecin provides an efficient system to direct topoisomerase I mediated DNA cleavage to specific sites. These conjugates are equally as potent at targeting the enzyme to a single site in a DNA fragment as camptothecin conjugates of ligands that bind in the major groove (triplex-forming oligonucleotides).

Keywords: DNA cleavage; DNA recognition; antitumor agents; drug research; topoisomerase.

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