ArticleScientific reports2019
Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 34 citations in OpenAlex.
- A fission yeast-based platform for nematode PDE inhibitor discovery.Cellular signalling · 2026Article
- Structure-guided screening of FAR-1 antagonists with multi-stage anthelmintic activity.Antimicrobial agents and chemotherapy · 2026Article
- Design, synthesis, and biological evaluation of a focused pyrrolo- and pyrido-quinazolinone natural products-templated library for anti-fungal and anthelmintic activities.Bioorganic & medicinal chemistry · 2026Article
- Prediction and Prioritisation of Novel Anthelmintic Candidates from Public Databases Using Deep Learning and Available Bioactivity Data Sets.International journal of molecular sciences · 2025Article
- Discovery of Human PIM Kinase Inhibitors as a Class of Anthelmintic Drugs to Treat Intestinal Nematode Infections.ACS infectious diseases · 2025Article
- High-Throughput Screening of More Than 30,000 Compounds for Anthelmintics against Gastrointestinal Nematode Parasites.ACS infectious diseases · 2025Article
- Article
- Antifungal and Antiparasitic Activities of Metallocene-Containing Fluconazole Derivatives.ACS infectious diseases · 2024Article
- Getting around the roundworms: Identifying knowledge gaps and research priorities for the ascarids.Advances in parasitology · 2024Article
- Discovery of New Broad-Spectrum Anti-Infectives for Eukaryotic Pathogens Using Bioorganometallic Chemistry.Journal of medicinal chemistry · 2023Article
- A genome-scale metabolic model of parasitic whipworm.Nature communications · 2023Article
- Multivariate chemogenomic screening prioritizes new macrofilaricidal leads.Communications biology · 2023Article
- Identification of antiparasitic drug targets using a multi-omics workflow in the acanthocephalan model.BMC genomics · 2022Article
- Identification of enzymes that have helminth-specific active sites and are required for Rhodoquinone-dependent metabolism as targets for new anthelmintics.PLoS neglected tropical diseases · 2021Article
- A fragment-based approach identifies an allosteric pocket that impacts malate dehydrogenase activity.Communications biology · 2021Article
- An Integrated Approach to Identify New Anti-Filarial Leads to Treat River Blindness, a Neglected Tropical Disease.Pathogens (Basel, Switzerland) · 2021Article
- Use of a Fission Yeast Platform to Identify and Characterize Small Molecule PDE Inhibitors.Frontiers in pharmacology · 2021Review
- Rapid determination of nematode cell and organ susceptibility to toxic treatments.International journal for parasitology. Drugs and drug resistance · 2020Article
- Article
- De novo identification of toxicants that cause irreparable damage to parasitic nematode intestinal cells.PLoS neglected tropical diseases · 2020Article
Corrections and comments
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Authors and funding
11 authors at 6 institutions in 1 country.
Funding
Abstract
Targeting chokepoint enzymes in metabolic pathways has led to new drugs for cancers, autoimmune disorders and infectious diseases. This is also a cornerstone approach for discovery and development of anthelmintics against nematode and flatworm parasites. Here, we performed omics-driven knowledge-based identification of chokepoint enzymes as anthelmintic targets. We prioritized 10 of 186 phylogenetically conserved chokepoint enzymes and undertook a target class repurposing approach to test and identify new small molecules with broad spectrum anthelmintic activity. First, we identified and tested 94 commercially available compounds using an in vitro phenotypic assay, and discovered 11 hits that inhibited nematode motility. Based on these findings, we performed chemogenomic screening and tested 32 additional compounds, identifying 6 more active hits. Overall, 6 intestinal (single-species), 5 potential pan-intestinal (whipworm and hookworm) and 6 pan-Phylum Nematoda (intestinal and filarial species) small molecule inhibitors were identified, including multiple azoles, Tadalafil and Torin-1. The active hit compounds targeted three different target classes in humans, which are involved in various pathways, including carbohydrate, amino acid and nucleotide metabolism. Last, using representative inhibitors from each target class, we demonstrated in vivo efficacy characterized by negative effects on parasite fecundity in hamsters infected with hookworms.
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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.