公开(公告)号：US20080015145A1

公开(公告)日：2008-01-17

申请号：US11484364

申请日：2006-07-11

申请人： Maria Gyongyossy-Issa ,  Dana V. Devine ,  Iren Constantinescu ,  William Campbell ,  Carlos del Carpio Munoz

发明人： Maria Gyongyossy-Issa ,  Dana V. Devine ,  Iren Constantinescu ,  William Campbell ,  Carlos del Carpio Munoz

IPC分类号： A61K38/17 ,  C07K14/705

CPC分类号： C07K14/705 ,  A61K38/00 ,  A61K47/60

摘要： Mimotope receptors and inhibitors employ peptide mimics that mimic the shape and function of natural receptors and ligands, thus providing synthetic binding sites for ligands and receptors. Receptor mimics can be attached to carriers, such as liposomes, to act as synthetic platelets, for example, by providing binding sites for binding to other (natural or synthetic) platelets or to the endothelium. Synthetic platelets would have virtually limitless shelf life and would not require disease screening prior to transfusion, thereby providing a solution to the perpetual platelet shortages, as well as the safety and storage issues associated with natural blood platelets. Mimotope inhibitors (either free-molecule receptors or ligands) can act as antithrombotics by inhibiting platelet-platelet or platelet-endothelium interactions. Ligand mimics are preferably D-peptides that resist proteolytic degradation. Furthermore, these ligand mimics can also be attached to carriers for resisting excretion, thus forming the basis for a new class of antithrombotic drugs.

摘要翻译： 模拟表位受体和抑制剂使用模仿天然受体和配体的形状和功能的肽模拟物，从而为配体和受体提供合成结合位点。 受体模拟物可以连接到载体，例如脂质体，以作为合成血小板，例如通过提供与其他（天然或合成的）血小板或内皮结合的结合位点。 合成血小板将具有几乎无限的保质期，并且在输血之前不需要疾病筛查，从而提供对永久血小板缺乏症以及与天然血小板相关的安全和储存问题的解决方案。 模拟表位抑制剂（自由分子受体或配体）可以通过抑制血小板 - 血小板或血小板 - 内皮相互作用而作为抗血栓形成。 配体模拟物优选是抵抗蛋白水解降解的D肽。 此外，这些配体模拟物也可以连接到载体以抵抗排泄，从而形成新类型抗血栓药物的基础。