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Al-Riyami, Lamyaa, Pineda, Miguel A., Rzepecka, Justyna, Huggan, Judith K., Khalaf, Abedawn I., Suckling, Colin J., Scott, Fraser J., Rodgers, David T., Harnett, Margaret M. and Harnett, William (2013) Designing Anti-inflammatory Drugs from Parasitic Worms: A Synthetic Small Molecule Analogue of theAcanthocheilonema viteaeProduct ES-62 Prevents Development of Collagen-Induced Arthritis. Journal of Medicinal Chemistry, 56 (24). pp. 9982-10002. ISSN 0022-2623
Metadata only available from this repository.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
| Item Type: | Article |
|---|---|
| Subjects: | Q Science > Q Science (General) |
| Schools: | School of Applied Sciences |
| Depositing User: | Fraser Scott |
| Date Deposited: | 15 Aug 2017 10:53 |
| Last Modified: | 27 Mar 2018 13:15 |
| URI: | http://eprints.hud.ac.uk/id/eprint/32653 |
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