ArticlePLoS neglected tropical diseases2021
Identification of novel modulators of a schistosome transient receptor potential channel targeted by praziquantel.
Article in PLoS neglected tropical diseases, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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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
14 citing papers in PubMed, 23 citations in OpenAlex.
- Novel 1ACS infectious diseases · 2026Article
- Target-Based Design of Praziquantel Analogs at Cestode TRPMACS infectious diseases · 2025Article
- SARS-CoV-2 MSLAS discovery : advancing life sciences R & D · 2024Article
- Target-based discovery of a broad-spectrum flukicide.Nature structural & molecular biology · 2024Article
- Progress interrogating TRPMPZQ as the target of praziquantel.PLoS neglected tropical diseases · 2024Review
- TRP drop, TRP drop: a steady patter of anti-schistosomal target illumination.Frontiers in parasitology · 2024Review
- The Anthelmintic Activity of Praziquantel Analogs Correlates with Structure-Activity Relationships at TRPMACS medicinal chemistry letters · 2023Article
- Target-based discovery of a broad spectrum flukicide.bioRxiv : the preprint server for biology · 2023Article
- Metabolism of (R)-Praziquantel versus the Activation of a Parasite Transient Receptor Potential Melastatin Ion Channel.ChemMedChem · 2023Article
- Electrophysiological characterization of a schistosome transient receptor potential channel activated by praziquantel.International journal for parasitology · 2023Article
- Use the force, fluke: Ligand-independent gating of Schistosoma mansoni ion channel TRPMInternational journal for parasitology · 2023Article
- Natural variation in the binding pocket of a parasitic flatworm TRPM channel resolves the basis for praziquantel sensitivity.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Praziquantel activates a native cation current inFrontiers in parasitology · 2023Article
- Genetic analysis of praziquantel response in schistosome parasites implicates a transient receptor potential channel.Science translational medicine · 2021Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Given the worldwide burden of neglected tropical diseases, there is ongoing need to develop novel anthelmintic agents to strengthen the pipeline of drugs to combat these burdensome infections. Many diseases caused by parasitic flatworms are treated using the anthelmintic drug praziquantel (PZQ), employed for decades as the key clinical agent to treat schistosomiasis. PZQ activates a flatworm transient receptor potential (TRP) channel within the melastatin family (TRPMPZQ) to mediate sustained Ca2+ influx and worm paralysis. As a druggable target present in many parasitic flatworms, TRPMPZQ is a promising target for a target-based screening campaign with the goal of discovering novel regulators of this channel complex. Here, we have optimized methods to miniaturize a Ca2+-based reporter assay for Schistosoma mansoni TRPMPZQ (Sm.TRPMPZQ) activity enabling a high throughput screening (HTS) approach. This methodology will enable further HTS efforts against Sm.TRPMPZQ as well as other flatworm ion channels. A pilot screen of ~16,000 compounds yielded a novel activator of Sm.TRPMPZQ, and numerous potential blockers. The new activator of Sm.TRPMPZQ represented a distinct chemotype to PZQ, but is a known chemical entity previously identified by phenotypic screening. The fact that a compound prioritized from a phenotypic screening campaign is revealed to act, like PZQ, as an Sm.TRPMPZQ agonist underscores the validity of TRPMPZQ as a druggable target for antischistosomal ligands.
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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.