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Article

Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.

Journal of medicinal chemistry - 7 Apr 2005

Staker Bart L, Feese Michael D, Cushman Mark, Pommier Yves, Zembower David, Stewart Lance, Burgin Alex B

Abstract excerpt

Human topoisomerase I (top1) is the molecular target of a diverse set of anticancer compounds, including the camptothecins, indolocarbazoles, and indenoisoquinolines. These compounds bind to a transient top1-DNA covalent complex and inhibit the resealing of a single-strand nick that the enzyme creates to relieve superhelical tension in duplex DNA. (Hertzberg, R. P.; et al. Biochem. 1989, 28, 4629-4638. Hsiang, Y....

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Identifiers

PMID: 15801827
DOI: 10.1021/jm049146p

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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