ArticlePLoS neglected tropical diseases2015
Ergot Alkaloids (Re)generate New Leads as Antiparasitics.
Article in PLoS neglected tropical diseases, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed, 22 citations in OpenAlex.
- Article
- Article
- Schistosomiasis Drug Discovery in the Era of Automation and Artificial Intelligence.Frontiers in immunology · 2021Review
- Characterization of a new type of neuronal 5-HT G- protein coupled receptor in the cestode nervous system.PloS one · 2021Article
- Activation of transient receptor potential channel Sm.(Schistosoma mansoni)TRPMParasitology research · 2020Review
- Identification of annotated bioactive molecules that impair motility of the blood fluke Schistosoma mansoni.International journal for parasitology. Drugs and drug resistance · 2020Article
- The Journey to Discovering a Flatworm Target of Praziquantel: A Long TRP.Trends in parasitology · 2020Review
- CaCold Spring Harbor perspectives in biology · 2019Review
- Structure-activity profiling of alkaloid natural product pharmacophores against a Schistosoma serotonin receptor.International journal for parasitology. Drugs and drug resistance · 2018Article
- Coalescing beneficial host and deleterious antiparasitic actions as an antischistosomal strategy.eLife · 2018Article
- Activation of host transient receptor potential (TRP) channels by praziquantel stereoisomers.PLoS neglected tropical diseases · 2018Article
- Unique pharmacological properties of serotoninergic G-protein coupled receptors from cestodes.PLoS neglected tropical diseases · 2018Article
- The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand.Nature communications · 2017Article
- Utilizing the planarian voltage-gated ion channel transcriptome to resolve a role for a CaBiochimica et biophysica acta. Molecular cell research · 2017Article
- Kinetic profiling an abundantly expressed planarian serotonergic GPCR identifies bromocriptine as a perdurant antagonist.International journal for parasitology. Drugs and drug resistance · 2016Article
- Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist.International journal for parasitology. Drugs and drug resistance · 2016Article
- A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors.PLoS pathogens · 2016Article
- Physiological controls of large-scale patterning in planarian regeneration: a molecular and computational perspective on growth and form.Regeneration (Oxford, England) · 2016Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
Praziquantel (PZQ) is a key therapy for treatment of parasitic flatworm infections of humans and livestock, but the mechanism of action of this drug is unresolved. Resolving PZQ-engaged targets and effectors is important for identifying new druggable pathways that may yield novel antiparasitic agents. Here we use functional, genetic and pharmacological approaches to reveal that serotonergic signals antagonize PZQ action in vivo. Exogenous 5-hydroxytryptamine (5-HT) rescued PZQ-evoked polarity and mobility defects in free-living planarian flatworms. In contrast, knockdown of a prevalently expressed planarian 5-HT receptor potentiated or phenocopied PZQ action in different functional assays. Subsequent screening of serotonergic ligands revealed that several ergot alkaloids possessed broad efficacy at modulating regenerative outcomes and the mobility of both free living and parasitic flatworms. Ergot alkaloids that phenocopied PZQ in regenerative assays to cause bipolar regeneration exhibited structural modifications consistent with serotonergic blockade. These data suggest that serotonergic activation blocks PZQ action in vivo, while serotonergic antagonists phenocopy PZQ action. Importantly these studies identify the ergot alkaloid scaffold as a promising structural framework for designing potent agents targeting parasitic bioaminergic G protein coupled receptors.
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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.