莱克DC-SIGN的非碳水化合物抑制剂
M Jack Borrok1, Laura L Kiessling
1Department of Biochemistry and Chemistry, University of Wisconsin, Madison, WI 53706, USA.
Journal of the American Chemical Society
|October 2, 2007
概括
研究人员确定了树突细胞特异性细胞间粘附分子3-抓 nonintegrin (DC-SIGN) 的强有力的非碳水化合物抑制剂. 这些化合物为研究DC-SIGN提供了新的途径.
科学领域:
- 免疫学 免疫学 免疫学
- 分子生物学分子生物学
- 药物发现 药物发现 药物发现
背景情况:
- 树突细胞特异性细胞间粘附分子3-抓取非整体素 (DC-SIGN) 是树突细胞上的C型讲蛋白.
- DC-SIGN调解细胞粘附和抗原呈现,并被HIV-1和Mycobacterium tuberculosis等病原体利用.
- 现有的DC-SIGN连接体通常以碳水化合物为基础,具有毫米分子抑制常数.
研究的目的:
- 为了识别DC-SIGN的有力单价联体.
- 开发新的小分子来探索DC-SIGN功能,并作为治疗指导.
主要方法:
- 开发一种基于高通量光的竞争分析.
- 对DC-SIGN的非碳水化合物小分子抑制剂进行查.
主要成果:
- 发现了强大的非碳水化合物小分子抑制剂,其IC50值处于微分子范围 (1.610微M).
- 这些抑制剂有效地阻断DC-SIGN-碳水化合物相互作用和DC-SIGN介导的细胞粘附.
结论:
- 新型非碳水化合物抑制剂为研究DC-SIGN提供了强大的工具.
- 这些化合物可以阐明DC-SIGN在病原和免疫功能中的作用.
- 针对DC-SIGN介导过程的潜在治疗应用.
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