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- W2483554889 abstract "Resistance has undermined the use of chloroquine and antifolates in malaria treatment and is threatening the future use of current front-line therapies based on artemisinin combination therapy. The need for new antimalarial drugs is being addressed with cell-based and targeted inhibitor screens. This chapter discusses the discovery of potent inhibitors of two new drug targets phosphatidylinositol-4 kinase and elongation factor 2 identified following phenotypic screens. It reviews studies of N-myristoyltransferase (NMT) in Plasmodium, which have led to the validation of NMT as a drug target in malaria, the discovery and development of new lead compounds, and insights into the role of protein myristoylation in these parasites. Inhibitors that target the folate biosynthesis pathway of the parasite, including pyrimethamine, cycloguanil, and sulfadoxine, have also been widely used. The selective inhibitors emerging from these drug discovery programs have been used as chemical tools to probe parasite cell biology." @default.
- W2483554889 created "2016-08-23" @default.
- W2483554889 creator A5059682608 @default.
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- W2483554889 date "2016-07-25" @default.
- W2483554889 modified "2023-10-12" @default.
- W2483554889 title "<i>N</i> ‐Myristoyltransferase as a Target for Drug Discovery in Malaria" @default.
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- W2483554889 doi "https://doi.org/10.1002/9783527694082.ch12" @default.
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