ArticleJournal of medicinal chemistry2013
Designing anti-inflammatory drugs from parasitic worms: a synthetic small molecule analogue of the Acanthocheilonema viteae product ES-62 prevents development of collagen-induced arthritis.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.
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Who cites it
47 citing papers in PubMed, 92 citations in OpenAlex.
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- Characterization and ligand binding properties of a fatty acid- and retinol- binding protein (Hp-FAR-2) from Heligmosomoides polygyrus.PLoS neglected tropical diseases · 2025Article
- A secreted fatty acid- and retinol- binding protein frombioRxiv : the preprint server for biology · 2025Article
- Helminth Coinfections Modulate Disease Dynamics and Vaccination Success in the Era of Emerging Infectious Diseases.Vaccines · 2025Review
- Epigenetic changes induced by parasitic worms and their excretory-secretory products.Biochemical Society transactions · 2024Review
- The allure of targets for novel drugs.RSC medicinal chemistry · 2024Review
- Reduction in creatine metabolites in macrophages exposed to small molecule analogues of the anti-inflammatory parasitic worm product ES-62.Parasite immunology · 2024Article
- Development of Recyclable Polystyrene-Supported Phosphonic Acid Resins for Carbohydrate Immobilization and Glycosylation.The Journal of organic chemistry · 2023Article
- Protection against lung pathology during obesity-accelerated ageing in mice by the parasitic worm product ES-62.Frontiers in immunology · 2023Article
- The parasitic worm product ES-62 protects the osteoimmunology axis in a mouse model of obesity-accelerated ageing.Frontiers in immunology · 2022Article
- Suppression of inflammatory arthritis by the parasitic worm product ES-62 is associated with epigenetic changes in synovial fibroblasts.PLoS pathogens · 2021Article
- Selective Esterification of Phosphonic Acids.Molecules (Basel, Switzerland) · 2021Article
- Stability of housekeeping genes in inflamed joints of spontaneous and collagen-induced arthritis in DBA/1 mice.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2021Article
- Cytohesin-2/ARNO: A Novel Bridge Between Cell Migration and Immunoregulation in Synovial Fibroblasts.Frontiers in immunology · 2021Article
- Helminth Glycans at the Host-Parasite Interface and Their Potential for Developing Novel Therapeutics.Frontiers in molecular biosciences · 2021Review
- Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.Journal of medicinal chemistry · 2020Article
- Temperate Propolis Has Anti-Inflammatory Effects and Is a Potent Inhibitor of Nitric Oxide Formation in Macrophages.Metabolites · 2020Article
- Lipid profile of Trichinella papuae muscle-stage larvae.Scientific reports · 2020Article
- PreliminaryCells · 2020Article
- Synthesis, Antiproliferative Activity and Molecular Docking Studies of Novel Doubly Modified Colchicine Amides and Sulfonamides as Anticancer Agents.Molecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
Abstract
In spite of increasing evidence that parasitic worms may protect humans from developing allergic and autoimmune diseases and the continuing identification of defined helminth-derived immunomodulatory molecules, to date no new anti-inflammatory drugs have been developed from these organisms. We have approached this matter in a novel manner by synthesizing a library of drug-like small molecules based upon phosphorylcholine, the active moiety of the anti-inflammatory Acanthocheilonema viteae product, ES-62, which as an immunogenic protein is unsuitable for use as a drug. Following preliminary in vitro screening for inhibitory effects on relevant macrophage cytokine responses, a sulfone-containing phosphorylcholine analogue (11a) was selected for testing in an in vivo model of inflammation, collagen-induced arthritis (CIA). Testing revealed that 11a was as effective as ES-62 in protecting DBA/1 mice from developing CIA and mirrored its mechanism of action in downregulating the TLR/IL-1R transducer, MyD88. 11a is thus a novel prototype for anti-inflammatory drug development.
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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.