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Updated: Aug 12, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
[Inhibitors of DNA topoisomerases]
1Dept. of Bioengineering, Soka University Faculty of Engineering.
Abstract:
DNA topoisomerases are enzymes regulating the conformational state of DNA in every aspect of genetic processes by catalyzing transient cleavage and religation of DNA strands. The enzymes are targets of some of the important anticancer drugs. Many candidates of anticancer drugs are being screened via inhibition of the enzymes. In the present review, I discuss the role of DNA topoisomerases in genetic processes in mammalian cells, characteristics and mode of action of topoisomerase inhibitors, and resistance of tumor cells to the anticancer drugs.
Insights
DNA topoisomerases regulate DNA structure and are key targets for anticancer drugs. This review covers their role, inhibitors, and tumor resistance mechanisms.
Area of Science:
- Molecular Biology
- Biochemistry
- Genetics
Context:
- DNA topoisomerases are essential enzymes that manage DNA topology.
- These enzymes are crucial for DNA replication, transcription, and repair.
- They are validated targets for numerous anticancer therapies.
Purpose:
- To review the critical roles of DNA topoisomerases in mammalian genetic processes.
- To describe the characteristics and mechanisms of action of topoisomerase inhibitors.
- To discuss the phenomenon of tumor cell resistance to anticancer drugs targeting topoisomerases.
Summary:
- DNA topoisomerases (enzymes that manage DNA topology) are vital for cellular genetic processes.
- The review details their function, the mode of action of inhibitors used as anticancer drugs, and mechanisms of tumor resistance.
- Understanding these enzymes and their inhibitors is crucial for developing effective cancer treatments.
Impact:
- Provides a comprehensive overview of DNA topoisomerases and their significance in cancer therapy.
- Highlights the importance of topoisomerase inhibitors in oncology.
- Informs future research on overcoming drug resistance in cancer treatment.
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