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1. 发明申请

US20090232831A1 METHODS AND COMPOSITIONS FOR THE TREATMENT OR PREVENTION OF HUMAN IMMUNODEFICIENCY VIRUS INFECTION 审中-公开
标题翻译：治疗或预防人类免疫缺陷病毒感染的方法和组合
公开(公告)号：US20090232831A1
公开(公告)日：2009-09-17
申请号：US12338987
申请日：2008-12-18
申请人： Chi-Huey Wong , Sheng-Kai Wang , Pi-Hui Liang
发明人： Chi-Huey Wong , Sheng-Kai Wang , Pi-Hui Liang
IPC分类号： A61K39/42 , A61K31/715 , C07H1/00 , C12Q1/70
CPC分类号： A61K31/715 , A61K39/00 , G01N33/56988 , G01N33/6854 , G01N2400/00 , G01N2500/04
摘要： A conserved cluster of oligomannose glycans on gp120 has been identified as the epitope recognized by the broadly HIV-1-neutralizing monoclonal antibody 2G12. Oligomannose glycans are also the ligands for DC-SIGN, a C-type lectin found on the surface of dendritic cells. Multivalency is fundamental for carbohydrate-protein interactions, and mimicking of the high glycan density on the virus surface has become essential for designing carbohydrate-based HIV vaccines and antiviral agents. Synthesis of oligomannose dendrons, which display multivalent oligomannoses in high density, and characterize their interaction with 2G12 and DC-SIGN by a glycan microarray binding assay is disclosed. These glycodendrons inhibit the binding of gp120 to 2G12 and recombinant dimeric DC-SIGN with IC50 in the nanomolar range. A second-generation Man9 dendron was identified as a potential immunogen for HIV vaccine development and as a potential antiviral agent.
摘要翻译：已经鉴定了gp120上寡聚糖单糖聚糖的保守簇，被广泛的HIV-1中和单克隆抗体2G12识别为表位。寡聚甘露糖聚糖也是DC-SIGN的配体，DC-SIGN是树突细胞表面上发现的C型凝集素。多值是碳水化合物 - 蛋白质相互作用的基础，并且模仿病毒表面上的高聚糖密度对于设计基于碳水化合物的HIV疫苗和抗病毒剂已变得至关重要。公开了通过聚糖微阵列结合测定法显示高密度多价寡糖单糖的寡甘露糖树突的合成，并表征其与2G12和DC-SIGN的相互作用。这些甘草酮抑制gp120与2G12的结合和重组二聚体DC-SIGN，其IC50在纳摩尔范围。第二代Man9树突被鉴定为HIV疫苗开发的潜在免疫原，并被认为是潜在的抗病毒剂。

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