ArticleInternational journal for parasitology. Drugs and drug resistance2015
Identification of β-hematin inhibitors in the MMV Malaria Box.
Article in International journal for parasitology. Drugs and drug resistance, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- The Human Chk1 Inhibitor CHIR-124 Shows Multistage Activity against the Human Malaria ParasiteACS chemical biology · 2026Article
- Photopharmacology of Quinoline and Benzimidazole Azobenzene-Based Photoswitchable β‑Hematin Inhibitors.ACS omega · 2026Article
- Ferrocenyl Quinoline-Benzimidazole Hybrids: A Multistage Strategy to Combat Drug-Resistant Malaria.Inorganic chemistry · 2025Article
- The Medicines for Malaria Venture Malaria Box contains inhibitors of protein secretion in Plasmodium falciparum blood stage parasites.Traffic (Copenhagen, Denmark) · 2022Article
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- Heme Detoxification in the Malaria Parasite: A Target for Antimalarial Drug Development.Accounts of chemical research · 2021Review
- Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway inJournal of medicinal chemistry · 2021Article
- A Diverse Range of Hemozoin Inhibiting Scaffolds Act onACS infectious diseases · 2021Article
- Lapatinib, Nilotinib and Lomitapide Inhibit Haemozoin Formation in Malaria Parasites.Molecules (Basel, Switzerland) · 2020Article
- Virtual screening as a tool to discover new β-haematin inhibitors with activity against malaria parasites.Scientific reports · 2020Article
- The relative rate of kill of the MMV Malaria Box compounds provides links to the mode of antimalarial action and highlights scaffolds of medicinal chemistry interest.The Journal of antimicrobial chemotherapy · 2020Article
- Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles.RSC medicinal chemistry · 2020Article
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- Antimalarial activity of Malaria Box Compounds against Plasmodium falciparum clinical isolates.International journal for parasitology. Drugs and drug resistance · 2017Article
- Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery.Antimicrobial agents and chemotherapy · 2017Article
- Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active againstACS medicinal chemistry letters · 2017Article
- Metabolomics-Based Screening of the Malaria Box Reveals both Novel and Established Mechanisms of Action.Antimicrobial agents and chemotherapy · 2016Article
- Metabolomic Profiling of the Malaria Box Reveals Antimalarial Target Pathways.Antimicrobial agents and chemotherapy · 2016Article
- Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum.Journal of medicinal chemistry · 2016Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
The Malaria Box, assembled by the Medicines for Malaria Venture, is a set of 400 structurally diverse, commercially available compounds with demonstrated activity against blood-stage Plasmodium falciparum. The compounds are a representative subset of the 20,000 in vitro antimalarials identified from the high-throughput screening efforts of St. Jude Children's Research Hospital (TN, USA), Novartis and GlaxoSmithKline. In addition, a small set of active compounds from commercially available libraries was added to this group, but it has not previously been published. Elucidation of the biochemical pathways on which these compounds act is a major challenge; therefore, access to these compounds has been made available free of charge to the investigator community. Here, the Malaria Box compounds were tested for activity against the formation of β-hematin, a synthetic form of the heme detoxification biomineral, hemozoin. Further, the mechanism of action of these compounds within the malaria parasite was explored. Ten of the Malaria Box compounds demonstrated significant inhibition of β-hematin formation. In this assay, dose-response data revealed IC50 values ranging from 8.7 to 22.7 μM for these hits, each of which is more potent than chloroquine (a known inhibitor of hemozoin formation). The in vitro antimalarial activity of these ten hits was confirmed in cultures of the chloroquine sensitive D6 strain of the parasite resulting in IC50 values of 135-2165 nM, followed by testing in the multidrug resistant strain, C235. Cultures of P. falciparum (D6) were then examined for their heme distribution following treatment with nine of the commercially available confirmed compounds, seven of which disrupted the hemozoin pathway.
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