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Article

The mechanism of topoisomerase I poisoning by a camptothecin analog.

Proceedings of the National Academy of Sciences of the United States of America - 26 Nov 2002

Staker Bart L, Hjerrild Kathryn, Feese Michael D, Behnke Craig A, Burgin Alex B, Stewart Lance

Abstract excerpt

We report the x-ray crystal structure of human topoisomerase I covalently joined to double-stranded DNA and bound to the clinically approved anticancer agent Topotecan. Topotecan mimics a DNA base pair and binds at the site of DNA cleavage by intercalating between the upstream (-1) and downstream (+1) base pairs. Intercalation displaces the downstream DNA, thus preventing religation of the cleaved strand. By...

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Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

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Identifiers

PMID: 12426403
DOI: 10.1073/pnas.242259599
PMCID: PMC137726

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Source receipt: pubmed, retrieved 7 Sept 2026.

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