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1. 发明申请

US20060116325A1 Methods and compositions for inhibiting hiv-coreceptor interactions 审中-公开
标题翻译：用于抑制HIV感受器相互作用的方法和组合物
公开(公告)号：US20060116325A1
公开(公告)日：2006-06-01
申请号：US10468182
申请日：2002-02-15
申请人： Oleg Chertov , Joost Oppenheim , Xin Chen , Connor McGrath , Raymond Sowder , Jacek Lubkowski , Michele Wetzel , Thomas Rogers
发明人： Oleg Chertov , Joost Oppenheim , Xin Chen , Connor McGrath , Raymond Sowder , Jacek Lubkowski , Michele Wetzel , Thomas Rogers
IPC分类号： A61K38/10
CPC分类号： A61K38/162 , A61K39/12 , A61K39/21 , C07K14/005 , C12N2740/16122 , C12N2740/16134
摘要： Novel methods and compositions are provided for inhibiting interactions between human immunodeficiency viruses (HIVs) and viral coreceptors, including CXCR4 and/or CCR5 coreceptors. The anti-coreceptor binding agent includes a novel peptide portion of the gp120 envelope protein of HIV-1, as well as peptide analogs and mimetics of this peptide, that specifically binds to, or modulates activity of, the coreceptors(s). The anti-coreceptor binding agent is useful as a prophylactic or therapeutic treatment to prevent or inhibit HIV binding to a susceptible cell and thereby reduces infection and/or moderates or treats related diseases. In alternative embodiments, the peptides, analogs and mimetics are effective to inhibit direct co-receptor binding by HIV virus, coreceptor binding by HIV gp120 proteins or peptides, HIV fusion with target host cells, HIV virion entry into host cells, HIV replication, and HIV transmission between cells and hosts. In more detailed embodiments, the anti-coreceptor binding agents of the invention are multi-tropic by exhibiting activity against HIV interactions with multiple, CXCR4 and CCR5, coreceptors.
摘要翻译：提供新的方法和组合物用于抑制人免疫缺陷病毒（HIV）和病毒共同受体（包括CXCR4和/或CCR5共受体）之间的相互作用。抗感受器结合剂包括HIV-1的gp120包膜蛋白的新肽部分，以及该肽的肽类似物和模拟物，其特异性结合或调节共受体的活性。抗感受器结合剂可用作预防或治疗性治疗以预防或抑制HIV与敏感细胞的结合，从而降低感染和/或调节或治疗相关疾病。在替代实施方案中，肽，类似物和模拟物有效抑制HIV病毒的直接共受体结合，HIV gp120蛋白或肽的共受体结合，与靶宿主细胞的HIV融合，进入宿主细胞的HIV病毒体，HIV复制和细胞和宿主之间的HIV传播。在更详细的实施方案中，本发明的抗共感受体结合剂通过展现针对HIV与多种CXCR4和CCR5共受体的相互作用的活性而呈多向性。

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