ArticleACS chemical biology2011
A chemical genomic analysis of decoquinate, a Plasmodium falciparum cytochrome b inhibitor.
Article in ACS chemical biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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
59 citing papers in PubMed, 96 citations in OpenAlex.
- Structure, assembly and inhibition of the Toxoplasma gondii respiratory chain supercomplex.Nature structural & molecular biology · 2025Article
- The Thienopyrimidinone Gamhépathiopine Targets the QACS infectious diseases · 2025Article
- Improvement of the Solubility, Permeability, and Pharmacological Activity of Decoquinate-Loaded Hydroxypropyl-Pharmaceuticals (Basel, Switzerland) · 2025Article
- Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b.European journal of medicinal chemistry · 2024Article
- Comparative chemical genomics inProceedings of the National Academy of Sciences of the United States of America · 2024Article
- Distinct non-synonymous mutations in cytochrome b highly correlate with decoquinate resistance in apicomplexan parasite Eimeria tenella.Parasites & vectors · 2023Article
- Quinolone: a versatile therapeutic compound class.Molecular diversity · 2023Review
- In Vitro versus in Mice: Efficacy and Safety of Decoquinate and Quinoline-Pathogens (Basel, Switzerland) · 2023Article
- 7-ACS infectious diseases · 2023Article
- Preliminary Assessment of Intramuscular Depot of Lipid-Based Decoquinate Formulation for Long-Term Chemoprophylaxis of Malaria.Pharmaceutics · 2022Article
- Chemical and Pharmacological Properties of Decoquinate: A Review of Its Pharmaceutical Potential and Future Perspectives.Pharmaceutics · 2022Review
- Decoquinate liposomes: highly effective clearance of Plasmodium parasites causing severe malaria.Malaria journal · 2022Article
- The evaluation of ADME and pharmacokinetic properties of decoquinate derivatives for the treatment of malaria.Frontiers in pharmacology · 2022Article
- Assessment of the Activity of Decoquinate and Its Quinoline-Molecules (Basel, Switzerland) · 2021Article
- MalDA, Accelerating Malaria Drug Discovery.Trends in parasitology · 2021Review
- Complexome profile of Toxoplasma gondii mitochondria identifies divergent subunits of respiratory chain complexes including new subunits of cytochrome bc1 complex.PLoS pathogens · 2021Article
- Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites.Scientific reports · 2021Article
- Efforts Made to Eliminate Drug-Resistant Malaria and Its Challenges.BioMed research international · 2021Review
- Predicting Drug Resistance Using Deep Mutational Scanning.Molecules (Basel, Switzerland) · 2020Review
- The QACS infectious diseases · 2020Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 3 institutions in 1 country.
Funding
Abstract
Decoquinate has single-digit nanomolar activity against in vitro blood stage Plasmodium falciparum parasites, the causative agent of human malaria. In vitro evolution of decoquinate-resistant parasites and subsequent comparative genomic analysis to the drug-sensitive parental strain revealed resistance was conferred by two nonsynonymous single nucleotide polymorphisms in the gene encoding cytochrome b. The resultant amino acid mutations, A122T and Y126C, reside within helix C in the ubiquinol-binding pocket of cytochrome b, an essential subunit of the cytochrome bc(1) complex. As with other cytochrome bc(1) inhibitors, such as atovaquone, decoquinate has low nanomolar activity against in vitro liver stage P. yoelii and provides partial prophylaxis protection when administered to infected mice at 50 mg kg(-1). In addition, transgenic parasites expressing yeast dihydroorotate dehydrogenase are >200-fold less sensitive to decoquinate, which provides additional evidence that this drug inhibits the parasite's mitochondrial electron transport chain. Importantly, decoquinate exhibits limited cross-resistance to a panel of atovaquone-resistant parasites evolved to harbor various mutations in cytochrome b. The basis for this difference was revealed by molecular docking studies, in which both of these inhibitors were shown to have distinctly different modes of binding within the ubiquinol-binding site of cytochrome b.
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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.