ArticlePloS one2015
Screening the Medicines for Malaria Venture "Malaria Box" against the Plasmodium falciparum aminopeptidases, M1, M17 and M18.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 40 citations in OpenAlex.
- Synthesis and Evaluation of Peptoid-Based Compound Libraries as Inhibitors of Parasite Metallo-Aminopeptidases.ChemMedChem · 2026Article
- Discovery of small molecules with anthelmintic potential in the Medicines for Malaria Venture's COVID and Global Health Priority Boxes using an infrared-based assay for Caenorhabditis elegans motility.BMC research notes · 2025Article
- The Medicines for Malaria Venture Malaria Box contains inhibitors of protein secretion in Plasmodium falciparum blood stage parasites.Traffic (Copenhagen, Denmark) · 2022Article
- Driving antimalarial design through understanding of target mechanism.Biochemical Society transactions · 2020Review
- 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
- Structural characterization of plasmodial aminopeptidase: a combined molecular docking and QSAR-based in silico approaches.Molecular diversity · 2019Article
- Screening the Pathogen Box for Identification of New Chemical Agents with Anti-Antimicrobial agents and chemotherapy · 2019Article
- Structural Insights Into KeyFrontiers in microbiology · 2019Review
- Fragment-Based Screening of a Natural Product Library against 62 Potential Malaria Drug Targets Employing Native Mass Spectrometry.ACS infectious diseases · 2018Article
- Metallopeptidases of Toxoplasma gondii: in silico identification and gene expression.Parasite (Paris, France) · 2018Article
- Discovery of novel non-competitive inhibitors of mammalian neutral M1 aminopeptidase (APN).Biochimie · 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
- Biological characterization of chemically diverse compounds targeting the Plasmodium falciparum coenzyme A synthesis pathway.Parasites & vectors · 2016Article
- 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
- Characterization of aspartyl aminopeptidase from Toxoplasma gondii.Scientific reports · 2016Article
- Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.PLoS pathogens · 2016Article
- In Vitro Screening of the Open-Source Medicines for Malaria Venture Malaria Box Reveals Novel Compounds with Profound Activities against Theileria annulata Schizonts.Antimicrobial agents and chemotherapy · 2016Article
- Screening of the Open Source Malaria Box Reveals an Early Lead Compound for the Treatment of Alveolar Echinococcosis.PLoS neglected tropical diseases · 2016Article
- Bilayer Effects of Antimalarial Compounds.PloS one · 2015Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Malaria is a parasitic disease that remains a global health burden. The ability of the parasite to rapidly develop resistance to therapeutics drives an urgent need for the delivery of new drugs. The Medicines for Malaria Venture have compounds known for their antimalarial activity, but not necessarily the molecular targets. In this study, we assess the ability of the "MMV 400" compounds to inhibit the activity of three metalloaminopeptidases from Plasmodium falciparum, PfA-M1, PfA-M17 and PfM18 AAP. We have developed a multiplex assay system to allow rapid primary screening of compounds against all three metalloaminopeptidases, followed by detailed analysis of promising compounds. Our results show that there were no PfM18AAP inhibitors, whereas two moderate inhibitors of the neutral aminopeptidases PfA-M1 and PfA-M17 were identified. Further investigation through structure-activity relationship studies and molecular docking suggest that these compounds are competitive inhibitors with novel binding mechanisms, acting through either non-classical zinc coordination or independently of zinc binding altogether. Although it is unlikely that inhibition of PfA-M1 and/or PfA-M17 is the primary mechanism responsible for the antiplasmodial activity reported for these compounds, their detailed characterization, as presented in this work, pave the way for their further optimization as a novel class of dual PfA-M1/PfA-M17 inhibitors utilising non-classical zinc binding groups.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.