ArticleJournal of medicinal chemistry2014
Identification of an Atg8-Atg3 protein-protein interaction inhibitor from the medicines for Malaria Venture Malaria Box active in blood and liver stage Plasmodium falciparum parasites.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers, 2 of them syntheses that pooled it.
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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
31 citing papers in PubMed, 2 syntheses or guidelines pooled it, 49 citations in OpenAlex.
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- Guidelines for the use and interpretation of assays for monitoring autophagy (3rd edition).Autophagy · 2016Guideline
- Comparative 3D ultrastructure of Plasmodium falciparum gametocytes.Nature communications · 2025Article
- Drug discovery by targeting the protein-protein interactions involved in autophagy.Acta pharmaceutica Sinica. B · 2023Review
- Autophagy in protists and their hosts: When, how and why?Autophagy reports · 2023Article
- An Alternative Autophagy-Related Mechanism of Chloroquine Drug Resistance in the Malaria Parasite.Antimicrobial agents and chemotherapy · 2022Article
- The Pandemic Response Box─Accelerating Drug Discovery Efforts after Disease Outbreaks.ACS infectious diseases · 2022Article
- Article
- Modulation of autophagy as a therapeutic strategy forFrontiers in cellular and infection microbiology · 2022Review
- A Structural Approach into Drug Discovery Based on Autophagy.Life (Basel, Switzerland) · 2021Review
- Ubiquitin-Like Modifiers: Emerging Regulators of Protozoan Parasites.Biomolecules · 2020Review
- Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials.ACS infectious diseases · 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
- Leishmania donovani parasite requires Atg8 protein for infectivity and survival under stress.Cell death & disease · 2019Article
- Plastid-endomembrane connections in apicomplexan parasites.PLoS pathogens · 2019Review
- Characterization of the molecular mechanism of the autophagy-related Atg8-Atg3 protein interaction inThe Journal of biological chemistry · 2018Article
- Using Yeast Synthetic Lethality To Inform Drug Combination for Malaria.Antimicrobial agents and chemotherapy · 2018Article
- Structure-based drug design, synthesis and biological assays of P. falciparum Atg3-Atg8 protein-protein interaction inhibitors.Journal of computer-aided molecular design · 2018Article
- Characterization of Plasmodium Atg3-Atg8 Interaction Inhibitors Identifies Novel Alternative Mechanisms of Action in Toxoplasma gondii.Antimicrobial agents and chemotherapy · 2018Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Atg8 is a ubiquitin-like autophagy protein in eukaryotes that is covalently attached (lipidated) to the elongating autophagosomal membrane. Autophagy is increasingly appreciated as a target in diverse diseases from cancer to eukaryotic parasitic infections. Some of the autophagy machinery is conserved in the malaria parasite, Plasmodium. Although Atg8's function in the parasite is not well understood, it is essential for Plasmodium growth and survival and partially localizes to the apicoplast, an indispensable organelle in apicomplexans. Here, we describe the identification of inhibitors from the Malaria Medicine Venture Malaria Box against the interaction of PfAtg8 with its E2-conjugating enzyme, PfAtg3, by surface plasmon resonance. Inhibition of this protein-protein interaction prevents PfAtg8 lipidation with phosphatidylethanolamine. These small molecule inhibitors share a common scaffold and have activity against both blood and liver stages of infection by Plasmodium falciparum. We have derivatized this scaffold into a functional platform for further optimization.
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Registered trials
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.