ArticleNature communications2024
Eliminating malaria transmission requires targeting immature and mature gametocytes through lipoidal uptake of antimalarials.
Article in Nature communications, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Structure-Guided Optimization of Novel Inhibitors ofJournal of medicinal chemistry · 2026Article
- Ruthenium Complexes of Atovaquone Acting on Multiple Stages of theJournal of medicinal chemistry · 2026Article
- CAR-macrophage therapy: a novel strategy to overcome antimalarial drug resistance by targeting PfEMP1-mediated adhesion.Malaria journal · 2026Article
- Examination of Coligands in Mefloquine-Metal Complexes Reveals the Structural Determinants of Activity againstJournal of medicinal chemistry · 2026Article
- Protein Arginine Methyltransferase Inhibitors Target Multiple Stages ofACS infectious diseases · 2026Article
- Antiplasmodial Activity of Methylangolensate FromJournal of tropical medicine · 2026Article
- Novel Inhibitors ofJournal of medicinal chemistry · 2025Article
- Ferrocenyl Quinoline-Benzimidazole Hybrids: A Multistage Strategy to Combat Drug-Resistant Malaria.Inorganic chemistry · 2025Article
- The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4-Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria.Angewandte Chemie (International ed. in English) · 2025Article
- Medicinal Chemistry Progression of Sapanisertib, the Anticancer and DualJournal of medicinal chemistry · 2025Article
- Synthesis and SAR Studies of Acyl-Thiourea Platinum(II) Complexes Yield Analogs with Dual-Stage Antiplasmodium Activity.ACS medicinal chemistry letters · 2025Article
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13 authors.
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Abstract
Novel antimalarial compounds targeting both the pathogenic and transmissible stages of the human malaria parasite, Plasmodium falciparum, would greatly benefit malaria elimination strategies. However, most compounds affecting asexual blood stage parasites show severely reduced activity against gametocytes. The impact of this activity loss on a compound's transmission-blocking activity is unclear. Here, we report the systematic evaluation of the activity loss against gametocytes and investigate the confounding factors contributing to this. A threshold for acceptable activity loss between asexual blood stage parasites and gametocytes was defined, with near-equipotent compounds required to prevent continued gametocyte maturation and onward transmission. Target abundance is not predictive of gametocytocidal activity, but instead, lipoidal uptake is the main barrier of dual activity and is influenced by distinct physicochemical properties. This study provides guidelines for the required profiles of potential dual-active antimalarial agents and facilitates the development of effective transmission-blocking compounds.
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