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Updated: Dec 22, 2025

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Inhibitors of DNA Glycosylases as Prospective Drugs

Grigory V Mechetin1, Anton V Endutkin1, Evgeniia A Diatlova1

  • 1SB RAS Institute of Chemical Biology and Fundamental Medicine, 8 Lavrentieva Ave., Novosibirsk 630090, Russia.

International Journal of Molecular Sciences
|May 2, 2020
PubMed

Insights

DNA glycosylases initiate DNA repair to protect genomes. Inhibiting these enzymes shows promise for cancer therapy, but drugs are still in development.

Area of Science:

  • Biochemistry
  • Genetics
  • Pharmacology

Background:

  • DNA glycosylases are key enzymes initiating base excision repair (BER), a critical pathway for genomic stability.
  • BER inhibition is a promising therapeutic strategy for cancers with compromised DNA repair mechanisms, like BRCA-deficient tumors.
  • Targeting DNA glycosylases offers potential for treating various diseases, including cancer, neurodegenerative disorders, and infections.

Purpose of the Study:

  • To review the progress in validating DNA glycosylases as therapeutic targets.
  • To discuss current DNA glycosylase inhibitors and their development status.
  • To survey advancements in assays for screening potential glycosylase inhibitors.

Main Methods:

  • Literature review of studies on DNA glycosylase function and inhibition.
  • Analysis of therapeutic strategies targeting the base excision repair pathway.
  • Survey of high-throughput screening assays for DNA glycosylase activity.

Main Results:

  • DNA glycosylase inhibition is a validated strategy for specific cancer types.
  • Several classes of DNA glycosylase inhibitors have been described, but none have reached clinical trials.
  • Assay development is crucial for identifying and optimizing novel therapeutic compounds.

Conclusions:

  • DNA glycosylases represent a promising, yet underexplored, target class for pharmacological intervention.
  • Further development of specific inhibitors and robust screening assays is needed to advance therapeutic applications.
  • Targeting DNA glycosylases holds potential beyond cancer, including neurodegenerative diseases and infectious agents.
Keywords:
DNA glycosylasesDNA repairdrug targets

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