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DNA Topoisomerase I (Top1)

Target: Top1
Molecular classification: Enzyme, DNA topoisomerase, Isomerase

Overview

DNA topoisomerase I is a critical nuclear enzyme responsible for maintaining proper levels of supercoiling in cellular genomes by introducing transient single-strand breaks into duplex DNA. Its action ensures smooth progression through fundamental genetic processes while also serving as an important drug target in oncology due to its role in genome stability maintenance.

Other names: Topoisomerase (DNA) I

Mechanism of action

Single-strand cleavage/ligation via transesterification; trapping covalent complexes between enzyme and cleaved DNA ("TopI poisons") leading to cytotoxic lesions.

Biological functions

Regulation of DNA topologyDNA replicationTranscriptionRecombinationChromosome condensation/decondensationRelieving torsional stress

Disease associations

Cancer

Safety considerations

CytotoxicityMyelosuppressionGastrointestinal toxicity

Interacting drugs

Camptothecin derivatives (e.g., Topotecan, Irinotecan)

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