ArticleAntimicrobial agents and chemotherapy2005
3-Aminooxy-1-aminopropane and derivatives have an antiproliferative effect on cultured Plasmodium falciparum by decreasing intracellular polyamine concentrations.
Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 97 citations in OpenAlex.
- Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors.Journal of medicinal chemistry · 2025Article
- High Target Homology Does Not Guarantee Inhibition: Aminothiazoles Emerge as Inhibitors ofACS infectious diseases · 2024Article
- Chemoproteomics-based profiling reveals potential antimalarial mechanism of Celastrol by disrupting spermidine and protein synthesis.Cell communication and signaling : CCS · 2024Article
- 1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors.Scientific reports · 2023Article
- A non-canonical sensing pathway mediates Plasmodium adaptation to amino acid deficiency.Communications biology · 2023Article
- Article
- Robenidine Analogues Are Potent Antimalarials in Drug-ResistantACS infectious diseases · 2021Article
- Hydroxylamine Analogue of Agmatine: Magic Bullet for Arginine Decarboxylase.Biomolecules · 2020Article
- Novel Synthetic Polyamines Have Potent Antimalarial ActivitiesFrontiers in cellular and infection microbiology · 2019Article
- Polyamines in protozoan pathogens.The Journal of biological chemistry · 2018Review
- Inducing controlled cell cycle arrest and re-entry during asexual proliferation of Plasmodium falciparum malaria parasites.Scientific reports · 2018Article
- Uptake and metabolism of arginine impact Plasmodium development in the liver.Scientific reports · 2017Article
- Screening of potential targets in Plasmodium falciparum using stage-specific metabolic network analysis.Molecular diversity · 2015Article
- A novel inhibitor of Plasmodium falciparum spermidine synthase: a twist in the tail.Malaria journal · 2015Article
- Novel S-adenosyl-L-methionine decarboxylase inhibitors as potent antiproliferative agents against intraerythrocytic Plasmodium falciparum parasites.International journal for parasitology. Drugs and drug resistance · 2014Article
- Structural determinants of the 5'-methylthioinosine specificity of Plasmodium purine nucleoside phosphorylase.PloS one · 2014Article
- Vitamin B6-dependent enzymes in the human malaria parasite Plasmodium falciparum: a druggable target?BioMed research international · 2014Review
- Pharmacological potential of biogenic amine-polyamine interactions beyond neurotransmission.British journal of pharmacology · 2013Review
- In vitro activity of extracts and isolated polyphenols from West African medicinal plants against Plasmodium falciparum.Parasitology research · 2012Article
- Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities.Journal of medicinal chemistry · 2011Article
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8 authors at 3 institutions in 3 countries.
Funding
Abstract
The intraerythrocytic development of Plasmodium falciparum correlates with increasing levels of the polyamines putrescine, spermidine, and spermine in the infected red blood cells; and compartmental analyses revealed that the majority is associated with the parasite. Since depletion of cellular polyamines is a promising strategy for inhibition of parasite proliferation, new inhibitors of polyamine biosynthesis were tested for their antimalarial activities. The ornithine decarboxylase (ODC) inhibitor 3-aminooxy-1-aminopropane (APA) and its derivatives CGP 52622A and CGP 54169A as well as the S-adenosylmethionine decarboxlyase (AdoMetDC) inhibitors CGP 40215A and CGP 48664A potently affected the bifunctional P. falciparum ODC-AdoMetDC, with K(i) values in the low nanomolar and low micromolar ranges, respectively. Furthermore, the agents were examined for their in vitro plasmodicidal activities in 48-h incubation assays. APA, CGP 52622A, CGP 54169A, and CGP 40215A were the most effective, with 50% inhibitory concentrations below 3 microM. While the effects of the ODC inhibitors were completely abolished by the addition of putrescine, growth inhibition by the AdoMetDC inhibitor CGP 40215A could not be antagonized by putrescine or spermidine. Moreover, CGP 40215A did not affect the cellular polyamine levels, indicating a mechanism of action against P. falciparum independent of polyamine synthesis. In contrast, the ODC inhibitors led to decreased cellular putrescine and spermidine levels in P. falciparum, supporting the fact that they exert their antimalarial activities by inhibition of the bifunctional ODC-AdoMetDC.
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