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Researchers Identify Broad-Spectrum Inhibitors for Malaria Parasite's Key Protein Family

Two lead compounds targeting Plasmodium falciparum's FIKK kinases show promise in disrupting red blood cell infection and evading drug resistance.

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Overview

  • Scientists from the Francis Crick Institute and GIMM have uncovered the evolutionary role of FIKK kinases, a protein family essential for malaria parasite survival.
  • Analysis of over 2,000 genomes revealed strong conservation in 18 of 21 FIKK kinase genes, underscoring their critical role in infection and host adaptation.
  • One FIKK kinase was found to phosphorylate tyrosine, a unique capability among malaria parasites, enabling manipulation of host cell signaling pathways.
  • High-throughput screening with GlaxoSmithKline identified three inhibitory compounds, with two showing broad-spectrum effectiveness against FIKK kinases in vitro.
  • Researchers are now optimizing these compounds for safety and efficacy, aiming to develop next-generation antimalarials that combat drug resistance.