Second generation of fucose-based DC-SIGN ligands: affinity improvement and specificity versus Langerin

Second generation of fucose-based DC-SIGN ligands: affinity improvement and specificity versus Langerin
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DOI:
10.1039/c1ob05573a
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发表时间:
2011-01-01
影响因子:
3.2
通讯作者:
Bernardi, Anna
Bernardi, Anna
中科院分区:
化学3区
文献类型:
--
作者:
Andreini, Manuel;Doknic, Daniela;Bernardi, Anna

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DC-SIGN和Langerin是两种参与HIV感染初始步骤的C型凝集素:前者作为病毒附着因子,促进病毒入侵免疫系统,后者具有保护作用。使用常见的岩藻糖酰胺锚合成靶向DC-SIGN的潜在抗病毒化合物。通过SPR测试它们的DC-SIGN亲和力,发现其与天然配体Lewis-X(Le(X))的亲和力相似。还发现这些化合物对DC-SIGN具有选择性,并且仅与Langerin弱相互作用。这些分子是潜在的有用的治疗工具,对性传播的艾滋病毒感染。
DC-SIGN and Langerin are two C-type lectins involved in the initial steps of HIV infections: the former acts as a viral attachment factor and facilitates viral invasion of the immune system, the latter has a protective effect. Potential antiviral compounds targeted against DC-SIGN were synthesized using a common fucosylamide anchor. Their DC-SIGN affinity was tested by SPR and found to be similar to that of the natural ligand Lewis-X (Le(X)). The compounds were also found to be selective for DC-SIGN and to interact only weakly with Langerin. These molecules are potentially useful therapeutic tools against sexually transmitted HIV infection.