Research ArticleMalaria

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

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Science Translational Medicine  26 Apr 2017:
Vol. 9, Issue 387, eaad9735
DOI: 10.1126/scitranslmed.aad9735

A new antimalarial in the armamentarium

Paquet et al. screened a small-molecule library against the human malaria parasite, Plasmodium falciparum, and identified the 2-aminopyridine chemical class with potent activity. The optimized compound from this class, MMV390048, was active against multiple parasite life cycle stages, in both the mammalian host and the mosquito vector, and also killed drug-resistant parasites. MMV390048 killed the malaria parasite by blocking the parasite’s phosphatidylinositol 4-kinase (PI4K) and was able to protect monkeys from malaria infection. MMV390048 has potential as a new antimalarial drug that may contribute to global malaria eradication efforts.