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Article

Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay.

Molecular cancer therapeutics - 1 Jan 2009

Marchand Christophe, Lea Wendy A, Jadhav Ajit, Dexheimer Thomas S, Austin Christopher P, Inglese James, Pommier Yves, Simeonov Anton

Abstract excerpt

Tyrosyl-DNA phosphodiesterase I (Tdp1) resolves topoisomerase I (Top1)-DNA adducts accumulated from natural DNA damage as well as from the action of certain anticancer drugs. Tdp1 catalyzes the hydrolysis of the phosphodiester bond between the catalytic tyrosine residue of topoisomerase I and the DNA 3'-phosphate. Only a limited number of weak inhibitors have been reported for Tdp1, and there is an unmet need to...

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Identifiers

PMID: 19139134
DOI: 10.1158/1535-7163.MCT-08-0878
PMCID: PMC2676116

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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