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Repurposing Anticancer Drugs To Tackle Malaria.

Yohann Le Govic1,2, Sandrine Houzé3, Nicolas Papon4

  • 1Laboratoire de Parasitologie-Mycologie, Centre de Biologie Humaine, CHU Amiens Picardie - site Sud, Amiens, France.

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|May 1, 2021
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Summary

New antimalarial drugs targeting epigenetic enzymes are urgently needed due to drug resistance. Researchers discovered a selective Plasmodium falciparum histone deacetylase (HDAC) inhibitor effective against malaria parasites, offering hope for new treatments.

Keywords:
Plasmodium falciparumhistone deacetylasesmalariaquisinostatresistance

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Area of Science:

  • Malariology
  • Medicinal Chemistry
  • Epigenetics

Background:

  • Malaria remains a significant global health burden, necessitating new treatments due to widespread drug resistance.
  • Current antimalarial drugs, including artemisinin combination therapies (ACTs), face challenges from resistant Plasmodium parasites.
  • Novel therapeutic targets are crucial to overcome existing drug resistance and improve malaria control.

Purpose of the Study:

  • To identify and characterize novel antimalarial compounds targeting epigenetic pathways.
  • To discover selective inhibitors of Plasmodium falciparum histone deacetylase (HDAC) as a potential therapeutic strategy.
  • To evaluate the efficacy of identified compounds against various stages of the malaria parasite.

Main Methods:

  • Prioritization of compounds targeting epigenetic enzymes.
  • Discovery and characterization of a selective Plasmodium falciparum histone deacetylase (HDAC) inhibitor.
  • Assessment of inhibitor activity against different parasite life stages.

Main Results:

  • Identification of a selective inhibitor targeting a Plasmodium falciparum epigenetic enzyme.
  • Demonstration of high antimalarial activity of the inhibitor across various parasite stages.
  • Validation of histone deacetylase (HDAC) as a promising target for antimalarial drug development.

Conclusions:

  • Selective Plasmodium falciparum histone deacetylase (HDAC) inhibitors show significant potential as novel antimalarial agents.
  • Targeting epigenetic enzymes offers a promising strategy to combat drug-resistant malaria.
  • These findings may lead to new lead compounds for malaria treatment and elimination efforts.