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Approaches to repurposing reverse transcriptase antivirals in cancer

Richard Head1, Saiful Islam1, Jennifer H Martin2

  • 1Clinical and Health Sciences, University of South Australia, Adelaide, SA, Australia.

British Journal of Clinical Pharmacology
|May 28, 2025
PubMed

Insights

Reverse transcriptase inhibitors (RTIs) show anticancer potential by inducing cancer cell death through cell cycle arrest and immune response activation. These drugs suppress transposable elements like LINE-1, offering a new avenue for cancer treatment.

Area of Science:

  • Molecular Biology
  • Virology
  • Oncology

Background:

  • Cellular regulation involves non-terminal repeat retrotransposons and endogenous retroviruses.
  • Reverse transcriptase (RT) plays a key role in these processes.
  • RT inhibitors (RTIs) are explored for their potential in cancer therapy.

Purpose of the Study:

  • To review the role of RT inhibition in cellular regulation.
  • To discuss RT inhibitors (RTIs) as potential anticancer agents.
  • To explore the mechanisms by which RTIs induce cytotoxicity in cancer cells.

Main Methods:

  • Review of existing literature on RT inhibitors and their effects on cancer cells.
  • Analysis of the mechanisms of cytotoxicity induced by nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs).
  • Investigation into the role of LINE-1 elements and the cGAS-STING pathway in RTI-mediated effects.

Main Results:

  • RTIs, including NRTIs and NNRTIs, exhibit cytotoxicity in cancer cells, likely via endogenous RT inhibition.
  • RTIs induce cell cycle arrest and suppress transposable elements, notably inhibiting LINE-1.
  • LINE-1-derived DNA can activate the cGAS-STING pathway, promoting cell cycle arrest and immune responses.

Conclusions:

  • RTIs induce DNA strand breaks, incomplete retrotransposition, cell cycle arrest, and immune responses in cancer cells.
  • The relationship between PARP1, PARP2, DNA methylation, and LINE-1 retrotransposition warrants further investigation.
  • RT inhibitors like efavirenz show promise for preclinical evaluation as repurposed cancer drugs.
Keywords:
BRCAPARPantiviral drugscGAS‐STINGefavirenzrepurposingreverse transcriptase

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