2019
DOI: 10.1371/journal.pntd.0007693
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The repositioning of epigenetic probes/inhibitors identifies new anti-schistosomal lead compounds and chemotherapeutic targets

Abstract: BackgroundPraziquantel represents the frontline chemotherapy used to treat schistosomiasis, a neglected tropical disease (NTD) caused by infection with macro-parasitic blood fluke schistosomes. While this drug is safe, its inability to kill all schistosome lifecycle stages within the human host often requires repeat treatments. This limitation, amongst others, has led to the search for novel anti-schistosome replacement or combinatorial chemotherapies. Here, we describe a repositioning strategy to assess the a… Show more

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Cited by 28 publications
(30 citation statements)
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References 77 publications
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“…The results are shown in Fig 5. The cut-offs for defining hit compounds in this assay have been previously defined [37,55]. Nine compounds were hits in this assay for both motility and phenotype measurements.…”
Section: Resultsmentioning
confidence: 99%
See 2 more Smart Citations
“…The results are shown in Fig 5. The cut-offs for defining hit compounds in this assay have been previously defined [37,55]. Nine compounds were hits in this assay for both motility and phenotype measurements.…”
Section: Resultsmentioning
confidence: 99%
“…Auranofin was the positive control (screened at 10 μM). Dotted box indicates the threshold for activity in this assay: −0.15 for phenotype and −0.35 for motility; compounds must be below this threshold for both parameters to be considered a hit [37,55]. Compounds were screened in duplicate on two or three separate occasions and the data represents the average scores of these experiments.…”
Section: Resultsmentioning
confidence: 99%
See 1 more Smart Citation
“…It is now clear that epigenetic processes play important roles on schistosomes [81][82][83] . In fact, epigenetic mechanisms participate in schistosome phenotypic plasticity 84,85 , in egg production and adult worm viability 34,86,87 as well as in schistosomula survival [88][89][90][91][92] . DNA methylation, one of the most studied epigenetic mechanisms, has been detected in S. mansoni 15 , although the significance of DNA cytosine methylation (5mC) in this parasite has been somewhat controversial [93][94][95] .…”
Section: Discussionmentioning
confidence: 99%
“…Inhibitors and miRNAs from these orthologues were supplemented in the cultures of adults and schistosomula causing morphological changes, and the inhibition of a specific HMT resulted in a decrease in the epigenetic mark H3K36me associated with a reduction in motility and in the quantity of eggs produced. These assays open perspectives of treatment during the schistosomula stage ( Whatley et al, 2019 ).…”
Section: Potential Classes Of Epigenetic Biomarkers Applied To Schistmentioning
confidence: 99%