ArticleMolecular and biochemical parasitology2015
A constitutively active G protein-coupled acetylcholine receptor regulates motility of larval Schistosoma mansoni.
Article in Molecular and biochemical parasitology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- G protein-coupled receptor SmGPCR9 interacts with neuropeptides and controls spermatogenesis in Schistosoma mansoni.PLoS pathogens · 2026Article
- Bioaminergic signaling in parasitic flatworms: a perspective for linking GPCRs to behavior and drug discovery.Frontiers in parasitology · 2026Article
- Repurposing of Amiodarone for treatment of muscle phase of experimental trichinellosis spiralis.Journal of parasitic diseases : official organ of the Indian Society for Parasitology · 2025Article
- Rhodopsin orphan GPCR20 interacts with neuropeptides and directs growth, sexual differentiation, and egg production in femaleMicrobiology spectrum · 2024Article
- Form and Function in the Digenea, with an Emphasis on Host-Parasite and Parasite-Bacteria Interactions.Advances in experimental medicine and biology · 2024Review
- Annotation of G-Protein Coupled Receptors in the Genomes of Parasitic Blood Flukes.microPublication biology · 2023Article
- De novo transcriptome assembly and identification of G-Protein-Coupled-Receptors (GPCRs) in two species of monogenean parasites of fish.Parasite (Paris, France) · 2022Article
- Antiparasitic Properties of Cardiovascular Agents against Human Intravascular ParasitePharmaceuticals (Basel, Switzerland) · 2021Article
- Identification of annotated bioactive molecules that impair motility of the blood fluke Schistosoma mansoni.International journal for parasitology. Drugs and drug resistance · 2020Article
- Towards deorphanizing G protein-coupled receptors ofParasitology · 2020Article
- Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages.PLoS neglected tropical diseases · 2020Article
- Promethazine exhibits antiparasitic propertiesAntimicrobial agents and chemotherapy · 2019Article
- Chemotactic migration of newly excysted juvenile Clonorchis sinensis is suppressed by neuro-antagonists.PLoS neglected tropical diseases · 2019Article
- Octopamine signaling in the metazoan pathogenDisease models & mechanisms · 2018Article
- Profiling G protein-coupled receptors of Fasciola hepatica identifies orphan rhodopsins unique to phylum Platyhelminthes.International journal for parasitology. Drugs and drug resistance · 2018Article
- Tissue-specific transcriptome analyses provide new insights into GPCR signalling in adult Schistosoma mansoni.PLoS pathogens · 2018Review
- 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
- Comprehensive Transcriptome Analysis of Sex-Biased Expressed Genes Reveals Discrete Biological and Physiological Features of Male and Female Schistosoma japonicum.PLoS neglected tropical diseases · 2016Article
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4 authors.
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Abstract
The neuromuscular system of helminths controls a variety of essential biological processes and therefore represents a good source of novel drug targets. The neuroactive substance, acetylcholine controls movement of Schistosoma mansoni but the mode of action is poorly understood. Here, we present first evidence of a functional G protein-coupled acetylcholine receptor in S. mansoni, which we have named SmGAR. A bioinformatics analysis indicated that SmGAR belongs to a clade of invertebrate GAR-like receptors and is related to vertebrate muscarinic acetylcholine receptors. Functional expression studies in yeast showed that SmGAR is constitutively active but can be further activated by acetylcholine and, to a lesser extent, the cholinergic agonist, carbachol. Anti-cholinergic drugs, atropine and promethazine, were found to have inverse agonist activity towards SmGAR, causing a significant decrease in the receptor's basal activity. An RNAi phenotypic assay revealed that suppression of SmGAR activity in early-stage larval schistosomulae leads to a drastic reduction in larval motility. In sum, our results provide the first molecular evidence that cholinergic GAR-like receptors are present in schistosomes and are required for proper motor control in the larvae. The results further identify SmGAR as a possible candidate for antiparasitic drug targeting.
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