ArticleScientific reports2013
A whole cell pathway screen reveals seven novel chemosensitizers to combat chloroquine resistant malaria.
Article in Scientific reports, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 26 citations in OpenAlex.
- Article
- Two small-molecule inhibitors ofFrontiers in cellular and infection microbiology · 2023Article
- Targeting Artemisinin-Resistant Malaria by Repurposing the Anti-Hepatitis C Virus Drug Alisporivir.Antimicrobial agents and chemotherapy · 2022Article
- Chloroquine and hydroxychloroquine in the treatment of malaria and repurposing in treating COVID-19.Pharmacology & therapeutics · 2020Review
- Uptake of a fluorescently tagged chloroquine analogue is reduced in CQ-resistant compared to CQ-sensitive Plasmodium falciparum parasites.Malaria journal · 2019Article
- Current scenario and future strategies to fight artemisinin resistance.Parasitology research · 2019Review
- Plasmodium falciparum and Plasmodium vivax Demonstrate Contrasting Chloroquine Resistance Reversal Phenotypes.Antimicrobial agents and chemotherapy · 2017Article
- Overcoming Chloroquine Resistance in Malaria: Design, Synthesis, and Structure-Activity Relationships of Novel Hybrid Compounds.Antimicrobial agents and chemotherapy · 2016Article
- ω-Tbo-IT1-New Inhibitor of Insect Calcium Channels Isolated from Spider Venom.Scientific reports · 2015Article
- New insights into TB physiology suggest untapped therapeutic opportunities.Immunological reviews · 2015Review
- Validation of a chloroquine-induced cell death mechanism for clinical use against malaria.Cell death & disease · 2014Article
- Article
- A high-content phenotypic screen reveals the disruptive potency of quinacrine and 3',4'-dichlorobenzamil on the digestive vacuole of Plasmodium falciparum.Antimicrobial agents and chemotherapy · 2014Article
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Authors and funding
8 authors at 4 institutions in 4 countries.
Funding
Abstract
Due to the widespread prevalence of resistant parasites, chloroquine (CQ) was removed from front-line antimalarial chemotherapy in the 1990s despite its initial promise of disease eradication. Since then, resistance-conferring mutations have been identified in transporters such as the PfCRT, that allow for the efflux of CQ from its primary site of action, the parasite digestive vacuole. Chemosensitizing/chemoreversing compounds interfere with the function of these transporters thereby sensitizing parasites to CQ once again. However, compounds identified thus far have disappointing in vivo efficacy and screening for alternative candidates is required to revive this strategy. In this study, we propose a simple and direct means to rapidly screen for such compounds using a fluorescent-tagged CQ molecule. When this screen was applied to a small library, seven novel chemosensitizers (octoclothepin, methiothepin, metergoline, loperamide, chlorprothixene, L-703,606 and mibefradil) were quickly elucidated, including two which showed greater potency than the classical chemosensitizers verapamil and desipramine.
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Registered trials
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