ArticleThe Journal of antimicrobial chemotherapy2013
A member of the Ras oncogene family, RAP1A, mediates antileishmanial activity of monastrol.
Article in The Journal of antimicrobial chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
What it found
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Who cites it
5 citing papers in PubMed, 11 citations in OpenAlex.
- Genome-Wide Protein Interaction Analysis in Parasitic Gyrodactylus Flatworms-Fish Hosts System and Drug Target Identification.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Functional dissection of prenyltransferases reveals roles in endocytosis and secretory vacuolar sorting in type 2-ME49 strain ofVirulence · 2024Article
- Synthesis and Biological Evaluation of Tetrahydropyrimidine and Dihydropyridine Derivatives Against Leishmania Major.Acta parasitologica · 2022Article
- Cholesterol-lowering drug, in combination with chromium chloride, induces early apoptotic signals in intracellular L. donovani amastigotes, leading to death.Journal of biosciences · 2017Article
- Green Synthesis of Silver and Titanium Dioxide Nanoparticles Using Euphorbia prostrata Extract Shows Shift from Apoptosis to G0/G1 Arrest followed by Necrotic Cell Death in Leishmania donovani.Antimicrobial agents and chemotherapy · 2015Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectivesTo investigate the mode of action of monastrol in intracellular Leishmania.
methodsMicroarray experiments were conducted on an Affymetrix GeneChip(®) Human Genome U133 Plus 2.0 Array, to determine the genes that encode proteins related to pathological alterations of cell signalling pathways in intracellular Leishmania amastigotes in response to monastrol treatment.
resultsMonastrol induced unprenylated Rap1A in intracellular Leishmania when exposed to this anticancer drug at the IC50 (10 μM). Monastrol, known to cause mitotic arrest in cancer cells, inhibited Rap1A prenylation (geranylgeranylation) in intracellular Leishmania, which resulted in blockade at the G1 phase of the cell cycle. Growth inhibition, rather than apoptosis, was found to be the mechanism by which monastrol displays antileishmanial activity.
conclusionsPrenylation inhibitors (unprenylation) of cell signalling pathways can be exploited in Leishmania parasites as novel therapeutic tools.
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Registered trials
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