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Updated: May 24, 2026

A Simple, Rapid, and Quantitative Assay to Measure Repair of DNA-protein Crosslinks on Plasmids Transfected into Mammalian Cells
Published on: March 5, 2018
DNA interstrand cross-linking agents and their chemotherapeutic potential
L Brulikova1, J Hlavac, P Hradil
1Institute of Molecular and Translational Medicine, Department of Organic Chemistry, Faculty of Science, Palacky University, 17. listopadu 12, 771 46 Olomouc, Czech Republic.
Abstract:
DNA interstrand cross-linking (ICL) agents are an important group of cytotoxic drugs with the capability of binding covalently between two strands of DNA, thereby preventing vital processes such as replication or transcription in dividing cells. In anticancer therapy however, their potential is limited due to the resistance by various mechanisms. In order to develop highly effective antitumor drugs it is necessary to study both effective ICL formations and their subsequent repair mechanisms. This review presents an overview of development over the past decade and the use of both well-known and new DNA interstrand cross-linking agents. Their potential in applications especially as anticancer chemotherapeutics in the framework of current knowledge of repair mechanisms and development of combined chemotherapy is discussed.
Insights
DNA interstrand cross-linking agents are cytotoxic drugs that halt cancer cell division. Understanding their formation and repair mechanisms is key to developing effective anticancer therapies and overcoming drug resistance.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- DNA interstrand cross-linking (ICL) agents are cytotoxic drugs that bind DNA, inhibiting replication and transcription.
- Their therapeutic potential in anticancer therapy is often limited by cellular resistance mechanisms.
- Studying ICL agent efficacy and repair pathways is crucial for developing novel antitumor strategies.
Purpose of the Study:
- To review the development and application of DNA interstrand cross-linking agents over the past decade.
- To discuss their potential as anticancer chemotherapeutics in light of current knowledge.
- To explore the role of repair mechanisms and combined chemotherapy strategies.
Main Methods:
- Literature review of recent advancements in DNA interstrand cross-linking agents.
- Analysis of established and emerging ICL agents.
- Discussion of drug resistance and repair mechanisms.
- Exploration of combined chemotherapy approaches.
Main Results:
- Overview of well-known and novel DNA interstrand cross-linking agents.
- Insights into mechanisms of drug resistance.
- Understanding of DNA repair pathways relevant to ICL agents.
- Discussion on the potential of combined chemotherapy strategies.
Conclusions:
- Continued research into DNA interstrand cross-linking agents is vital for advancing cancer therapy.
- Targeting repair mechanisms and employing combination therapies can enhance the efficacy of ICL agents.
- Developing new ICL agents with improved efficacy and reduced resistance is a key goal.
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