Article

Cryo-EM structural analysis of human TOP1 trapping by eight clinical anticancer drugs

2026-08-07

Abstract excerpt

Human topoisomerase 1 (TOP1) resolves DNA supercoiling during replication and transcription and is a major target for anticancer therapy. TOP1 poisons exert cytotoxicity by stabilizing the TOP1-DNA cleavage complex (TOP1cc), thereby blocking DNA rejoining and generating lethal DNA damage. Several TOP1 poisons have been approved either as conventional therapeutics or as payloads in targeted delivery systems, and ma...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 8d5b9698-04f8-5837-a90b-55423bb7164b
DOI: 10.64898/2026.08.03.742490

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Cryo-EM structural analysis of human TOP1 trapping by eight clinical anticancer drugsDOI 10.64898/2026.08.03.742490Read

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

A structural model for the ternary cleavable complex formed between human topoisomerase I, DNA, and camptothecin.Semantic proximity Read

The indenoisoquinoline noncamptothecin topoisomerase I inhibitors: update and perspectivesSemantic proximity Read

Structural and Dynamical Effects Induced by the Anticancer Drug Topotecan on the Human Topoisomerase I – DNA ComplexSemantic proximity Read

DNA Topoisomerases and Their Poisoning by Anticancer and Antibacterial DrugsSemantic proximity Read

Targeting Topoisomerase I in the Era of Precision MedicineSemantic proximity Read

Structural basis of type II topoisomerase inhibition by the anticancer drug etoposide.Semantic proximity Read

Cryo-EM reveals a mechanism of USP1 inhibition through a cryptic binding siteSemantic proximity Read

Crystal structures of human topoisomerase I in covalent and noncovalent complexes with DNA.Semantic proximity Read

Cryo-EM structures reveal distinct mechanisms of inhibition of the human multidrug transporter ABCB1Semantic proximity Read

Molecular modeling studies of the DNA-topoisomerase I ternary cleavable complex with camptothecin.Semantic proximity Read

Structural insight of DNA topoisomerases I from camptothecin-producing plants revealed by molecular dynamics simulations.Semantic proximity Read