دورية
Sulfated Galactocerebrosides as Potential Antiinflammatory Agents
| العنوان: | Sulfated Galactocerebrosides as Potential Antiinflammatory Agents |
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| المؤلفون: | Marinier, A., Martel, A., Banville, J., Bachand, C., Remillard, R., Lapointe, P., Turmel, B., Menard, M., Harte, W. E., Jr., Wright, J. J. K., Todderud, G., Tramposch, K. M., Bajorath, J., Hollenbaugh, D., Aruffo, A. |
| المصدر: | Journal of Medicinal Chemistry; September 26, 1997, Vol. 40 Issue: 20 p3234-3247, 14p |
| مستخلص: | Native sulfatides, as well as many sulfated glycolipids, have been shown to avidly bind to the selectin receptors. In vivo, native sulfatides significantly block activity in selectin-dependent inflammatory responses. The fact that nonsulfated galactocerebrosides did not inhibit selectin-mediated adhesion identified a critical role for the anionic sulfate residue. We therefore initiated a program to evaluate the activity of position isomers. This study showed a binding selectivity for the positions 2 and 3 of the sulfate group on the carbohydrate ring as well as enhanced activity for the disulfated analogs. Furthermore, it was discovered that the attachment of lipophilic substituents on the carbohydrate ring was tolerated, consistent with the presence of a lipophilic pocket in the binding cavity. This resulted in compounds with a 6-fold increased potency. |
| قاعدة البيانات: | Supplemental Index |
Find this issue from the American Chemical Society | تدمد: | 00222623 15204804 |
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