期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 24, 页码 9982-10002出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm401251p
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资金
- Wellcome Trust
- Biotechnology and Biological Sciences Research Council UK
- Arthritis Research UK
- BBSRC [BB/E013929/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/E013929/1] Funding Source: researchfish
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 responses, a sulfone-containing phosphorylcholine analogue (11a) was selected for testing in 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. on relevant macrophage cytokine an in vivo model of inflammation,
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