ArticleAntimicrobial agents and chemotherapy2008
Sitamaquine sensitivity in Leishmania species is not mediated by drug accumulation in acidocalcisomes.
Article in Antimicrobial agents and chemotherapy, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 39 citations in OpenAlex.
- Are basic and lipophilic chain groups highly required in leishmanicidal quinolines to favor the phagolysosome accumulation?Frontiers in chemistry · 2025Article
- A comprehensive revision on the use of quinoline antimalarial drugs as leishmanicidal agents.Frontiers in chemistry · 2025Review
- 4-Aminoquinoline as a privileged scaffold for the design of leishmanicidal agents: structure-property relationships and key biological targets.Frontiers in chemistry · 2024Review
- The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates.Molecules (Basel, Switzerland) · 2022Review
- Lipid profile of Trichinella papuae muscle-stage larvae.Scientific reports · 2020Article
- Leishmania heme uptake involves LmFLVCRb, a novel porphyrin transporter essential for the parasite.Cellular and molecular life sciences : CMLS · 2020Article
- The Oral Antimalarial Drug Tafenoquine Shows Activity against Trypanosoma brucei.Antimicrobial agents and chemotherapy · 2015Article
- Design and synthesis of novel antileishmanial compounds.International journal of medicinal chemistry · 2015Article
- 4-amino bis-pyridinium derivatives as novel antileishmanial agents.Antimicrobial agents and chemotherapy · 2014Article
- Peptidomimetic and organometallic derivatives of primaquine active against Leishmania infantum.Antimicrobial agents and chemotherapy · 2012Article
- Discovery of safe and orally effective 4-aminoquinaldine analogues as apoptotic inducers with activity against experimental visceral leishmaniasis.Antimicrobial agents and chemotherapy · 2012Article
- The 8-aminoquinoline analogue sitamaquine causes oxidative stress in Leishmania donovani promastigotes by targeting succinate dehydrogenase.Antimicrobial agents and chemotherapy · 2011Article
- Sitamaquine overcomes ABC-mediated resistance to miltefosine and antimony in Leishmania.Antimicrobial agents and chemotherapy · 2011Article
- Antimony-resistant clinical isolates of Leishmania donovani are susceptible to paromomycin and sitamaquine.Antimicrobial agents and chemotherapy · 2011Article
- Sitamaquine as a putative antileishmanial drug candidate: from the mechanism of action to the risk of drug resistance.Parasite (Paris, France) · 2011Review
- Increased glycolytic ATP synthesis is associated with tafenoquine resistance in Leishmania major.Antimicrobial agents and chemotherapy · 2011Article
- Structures, targets and recent approaches in anti-leishmanial drug discovery and development.The open medicinal chemistry journal · 2011Article
- Tafenoquine, an antiplasmodial 8-aminoquinoline, targets leishmania respiratory complex III and induces apoptosis.Antimicrobial agents and chemotherapy · 2010Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sitamaquine (WR6026), an 8-aminoquinoline derivative, is a new antileishmanial oral drug. As a lipophilic weak base, it rapidly accumulates in acidic compartments, represented mainly by acidocalcisomes. In this work, we show that the antileishmanial action of sitamaquine is unrelated to its level of accumulation in these acidic vesicles. We have observed significant differences in sitamaquine sensitivity and accumulation between Leishmania species and strains, and interestingly, there is no correlation between them. However, there is a relationship between the levels of accumulation of sitamaquine and acidotropic probes, acidocalcisomes size, and polyphosphate levels. The Leishmania major AP3delta-null mutant line, in which acidocalcisomes are devoid of their usual polyphosphate and proton content, is unable to accumulate sitamaquine; however, both the parental strain and the AP3delta-null mutants showed similar sensitivities to sitamaquine. Our findings provide clear evidence that the antileishmanial action of sitamaquine is unrelated to its accumulation in acidocalcisomes.
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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.