ArticleAntimicrobial agents and chemotherapy2016
In Vitro Screening of the Open-Source Medicines for Malaria Venture Malaria Box Reveals Novel Compounds with Profound Activities against Theileria annulata Schizonts.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 1 of them a synthesis that pooled it.
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Who cites it
12 citing papers in PubMed, 1 synthesis or guideline pooled it, 16 citations in OpenAlex.
- Targeting piroplasmosis and theileriosis: New frontiers in drug development.Tropical animal health and production · 2025Pooled it
- Article
- Article
- Artemisinin derivatives induce oxidative stress leading to DNA damage and caspase-mediated apoptosis in Theileria annulata-transformed cells.Cell communication and signaling : CCS · 2023Article
- Tulathromycin and Diclazuril Lack Efficacy againstPathogens (Basel, Switzerland) · 2023Article
- Trifloxystrobin blocks the growth of Theileria parasites and is a promising drug to treat Buparvaquone resistance.Communications biology · 2022Article
- In Vitro Activities of MMV Malaria Box Compounds against the Apicomplexan ParasiteMolecules (Basel, Switzerland) · 2020Article
- Leveraging the Medicines for Malaria Venture malaria and pathogen boxes to discover chemical inhibitors of East Coast fever.International journal for parasitology. Drugs and drug resistance · 2019Article
- Endochin-Like Quinolones Exhibit Promising Efficacy AgainstFrontiers in veterinary science · 2018Article
- Metabolomic Profiling of the Malaria Box Reveals Antimalarial Target Pathways.Antimicrobial agents and chemotherapy · 2016Article
- Extensive Shared Chemosensitivity between Malaria and Babesiosis Blood-Stage Parasites.Antimicrobial agents and chemotherapy · 2016Article
- Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.PLoS pathogens · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Intracellular schizonts of the apicomplexans Theileria annulata and Theileria parva immortalize bovine leukocytes and thereby cause fatal diseases. The hydroxynaphthoquinone buparvaquone is currently the only option for the treatment of theileriosis, and resistance development has been reported. It is therefore tempting to investigate the repurposing of compounds effective against related apicomplexan parasites, such as Plasmodium Here, we present the results of a screen of 400 compounds included in the open-access Medicines for Malaria Venture (MMV) malaria box on TaC12 cells, a macrophage-derived cell line immortalized by T. annulata schizonts. Using a combination of the classical alamarBlue vitality assay and a recently developed quantitative reverse transcriptase real-time PCR method based on the Theileria TaSP gene, we have identified 5 compounds, characterized their effects on the ultrastructure of TaC12 cells, and investigated whether they easily induce resistance formation. Two compounds, the quinolinols MMV666022 and MMV666054, have 50% inhibitory concentrations (IC50s) of 0.5 and 0.2 μM on TaC12 cells and 5.3 and 5.2 μM on BoMac cells, respectively. Thus, with therapeutic indexes of 11 and 18, they represent promising leads for further development of antitheilerial chemotherapeutics.
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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.