ArticleParasites & vectors2017
Screening of the 'Stasis Box' identifies two kinase inhibitors under pharmaceutical development with activity against Haemonchus contortus.
Article in Parasites & vectors, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 27 citations in OpenAlex.
- Evaluation of Serum Supplementation on the Development ofInternational journal of molecular sciences · 2025Article
- A phenotypic screen of the Global Health Priority Box identifies an insecticide with anthelmintic activity.Parasites & vectors · 2024Article
- A High-Throughput Phenotypic Screen of the 'Pandemic Response Box' Identifies a Quinoline Derivative with Significant Anthelmintic Activity.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Image recognition based on deep learning inComputational and structural biotechnology journal · 2022Article
- The ATP bioluminescence assay: a new application and optimization for viability testing in the parasitic nematode Haemonchus contortus.Veterinary research · 2021Article
- Cell Death and Transcriptional Responses Induced in Larvae of the NematodePharmaceuticals (Basel, Switzerland) · 2021Article
- Three Small Molecule Entities (MPK18, MPK334 and YAK308) with Activity againstMolecules (Basel, Switzerland) · 2021Article
- Anthelmintic drug discovery: target identification, screening methods and the role of open science.Beilstein journal of organic chemistry · 2020Review
- Phenotypic screening of the 'Kurz-box' of chemicals identifies two compounds (BLK127 and HBK4) with anthelmintic activity in vitro against parasitic larval stages of Haemonchus contortus.Parasites & vectors · 2019Article
- Tetrahydroquinoxalines induce a lethal evisceration phenotype in Haemonchus contortus in vitro.International journal for parasitology. Drugs and drug resistance · 2019Article
- Interactive online application for the prediction, ranking and prioritisation of drug targets in Schistosoma haematobium.Parasites & vectors · 2018Article
- Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni.Parasites & vectors · 2018Article
- Addressing the most neglected diseases through an open research model: The discovery of fenarimols as novel drug candidates for eumycetoma.PLoS neglected tropical diseases · 2018Article
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundIn partnership with the Medicines for Malaria Venture (MMV), we screened a collection ('Stasis Box') of 400 compounds (which have been in clinical development but have not been approved for illnesses other than neglected infectious diseases) for inhibitory activity against Haemonchus contortus, in order to attempt to repurpose some of the compounds to parasitic nematodes.
methodsWe assessed the inhibition of compounds on the motility and/or development of exsheathed third-stage (xL3s) and fourth-stage (L4) larvae of H. contortus using a whole-organism screening assay.
resultsIn the primary screen, we identified compound MMV690767 (also known as SNS-032) that inhibited xL3 motility by ~70% at a concentration of 20 μM after 72 h as well as compound MMV079840 (also known as AG-1295), which induced a coiled xL3 phenotype, with ~50% inhibition on xL3 motility. Subsequently, we showed that SNS-032 (IC
conclusionsAlthough the two kinase inhibitors, SNS-032 and AG-1295, had moderate inhibitory activity on the motility or development of xL3s or L4s of H. contortus in vitro, further work needs to be undertaken to chemically alter these entities to achieve the potency and selectivity required for them to become nematocidal or nematostatic candidates.
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