ArticleInternational journal for parasitology. Drugs and drug resistance2015
Leishmania is not prone to develop resistance to tamoxifen.
Article in International journal for parasitology. Drugs and drug resistance, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
- Therapeutic effect of topical tamoxifen in murine cutaneous leishmaniasis caused byAntimicrobial agents and chemotherapy · 2024Article
- Multitarget Compounds for Neglected Diseases: A Review.Current drug targets · 2024Review
- Recent Advances in Chemotherapeutics for Leishmaniasis: Importance of the Cellular Biochemistry of the Parasite and Its Molecular Interaction with the Host.Pathogens (Basel, Switzerland) · 2023Review
- Antileishmanial Activity of Tamoxifen by Targeting Sphingolipid Metabolism: A Review.Clinical pharmacology : advances and applications · 2022Review
- Network-Based Approaches Reveal Potential Therapeutic Targets for Host-Directed Antileishmanial Therapy Driving Drug Repurposing.Microbiology spectrum · 2021Article
- Repositioning of Tamoxifen in Surface-Modified Nanocapsules as a Promising Oral Treatment for Visceral Leishmaniasis.Pharmaceutics · 2021Article
- Effect of DODAB Nano-Sized Cationic Bilayer Fragments againstMolecules (Basel, Switzerland) · 2020Article
- Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites.Microorganisms · 2020Review
- Coupling chemical mutagenesis to next generation sequencing for the identification of drug resistance mutations in Leishmania.Nature communications · 2019Article
- Tamoxifen activity against Plasmodium in vitro and in mice.Malaria journal · 2019Article
- Review
- Tamoxifen inhibits the biosynthesis of inositolphosphorylceramide in Leishmania.International journal for parasitology. Drugs and drug resistance · 2018Article
- Selective inhibition of RNA polymerase I transcription as a potential approach to treat African trypanosomiasis.PLoS neglected tropical diseases · 2017Article
- Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus.Parasites & vectors · 2016Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tamoxifen, an antineoplastic agent, is active in vitro and in vivo against the parasitic protozoa Leishmania. As part of our efforts to unravel this drug's mechanisms of action against the parasite and understand how resistance could arise, we tried to select tamoxifen-resistant Leishmania amazonensis. Three different strategies to generate tamoxifen resistant mutants were used: stepwise increase in drug concentration applied to promastigote cultures, chemical mutagenesis followed by drug selection and treatment of infected mice followed by selection of amastigotes. For amastigote selection, we employed a method with direct plating of parasites recovered from lesions into semi-solid media. Tamoxifen resistant parasites were not rescued by any of these methods. Miltefosine was used as a control in selection experiments and both stepwise selection and chemical mutagenesis allowed successful isolation of miltefosine resistant mutants. These findings are consistent with a multi-target mode of action to explain tamoxifen's leishmanicidal properties. Considering that drug resistance is a major concern in anti-parasitic chemotherapy, these findings support the proposition of using tamoxifen as a partner in drug combination schemes for the treatment of leishmaniasis.
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