Browsing by Author "Lafuente-Monasterio, Maria"

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    Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics
    (BioMed Central Ltd, 2014) Ghidelli-Disse, Sonja; Lafuente-Monasterio, Maria; Waterson, David; Witty, Michael; Younis, Yassir; Paquet, Tanya; Street, Leslie; Chibale, Kelly; Gamo-Benito, Francisco; Bantscheff, Marcus; Drewes, Gerard
    Most antimalarial drugs face decreased efficacy due to the emergence of resistant parasites. Therefore, the discovery of new antimalarial medicines is focused on new drugs that act by novel mechanisms and are active against different P. falciparum development stages. Screening of a focused compound library for antiparasitic activity, lead to identification of a novel class of compounds with activity against P. falciparum, 2-aminopyridines. The selected hits were validated and subjected to a lead optimization program resulting in the pre-clinical candidate MMV390048. Here we report an unbiased chemoproteomics strategy for the identification of targets of MMV390048.