Journal of medicinal chemistry, 2007-02, Vol.50 (3), p.585-589
2007
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and Evaluation of 1,2,3-Triazole Containing Analogues of the Immunostimulant α-GalCer
- Ist Teil von
- Journal of medicinal chemistry, 2007-02, Vol.50 (3), p.585-589
- Ort / Verlag
- Washington, DC: American Chemical Society
- Erscheinungsjahr
- 2007
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- α-GalCer is the first defined and most potent agonistic antigen of the T cell receptor of natural killer T cells. We have prepared a series of 1,2,3-triazole-containing α-GalCer analogues in which the lipid chain lengths have been incrementally varied. We found that this isosteric replacement of α-GalCer's amide moiety with triazole increases the IL-4 versus IFN-γ bias of released cytokines. The stimulatory effect was influenced by the length of the attached chain. In particular, the long-chained triazole analogues have a comparable stimulatory effect on cytokine production as α-GalCer and exhibit a stronger Th2 cytokine response.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm061243qTitel-ID: cdi_proquest_miscellaneous_68960320
- Format
- –
- Schlagworte
- Adjuvants, Immunologic - chemical synthesis, Adjuvants, Immunologic - chemistry, Adjuvants, Immunologic - pharmacology, Animals, Antigens, CD1 - chemistry, Antigens, CD1d, Biological and medical sciences, Cell Line, Tumor, Coculture Techniques, Galactosylceramides - chemical synthesis, Galactosylceramides - chemistry, Galactosylceramides - pharmacology, Humans, Hybridomas, Immunomodulators, Interferon-gamma - secretion, Interleukin-2 - secretion, Interleukin-4 - secretion, Medical sciences, Mice, Mice, Inbred C57BL, Models, Molecular, Pharmacology. Drug treatments, Rats, Receptors, Antigen, T-Cell - agonists, Spleen - cytology, Structure-Activity Relationship, Th2 Cells - immunology, Triazoles - chemical synthesis, Triazoles - chemistry, Triazoles - pharmacology