申请人:Alavita Pharmaceuticals, Inc.
公开号:EP1839670A2
公开(公告)日:2007-10-03
A modified annexin protein, preferably annexin V, is used to prevent thrombosis without increasing hemorrhage. Annexin binds to, phosphatidylserine on the outer surface of cell membranes, thereby preventing binding of the prothrombinase complex necessary for thrombus formation. It does not, however, affect platelet aggregation necessary for hemostasis. The modified annexin molecule can be a homodimer of annexin, an annexin molecule coupled to one or more polyethylene glycol chains, or an annexin molecule coupled to another protein. By increasing the molecular weight of annexin, the modified annexin is made to remain in circulation for sufficient time to provide a sustained therapeutic effect.
经修饰的附蛋白(最好是附蛋白 V)可用于防止血栓形成,而不会增加出血量。附件蛋白与细胞膜外表面的磷脂酰丝氨酸结合,从而阻止血栓形成所需的凝血酶原复合物的结合。不过,它不会影响止血所需的血小板聚集。修饰的附件蛋白分子可以是附件蛋白的同源二聚体、与一个或多个聚乙二醇链偶联的附件蛋白分子或与另一种蛋白质偶联的附件蛋白分子。通过增加附件素的分子量,可使修饰的附件素在血液循环中保持足够的时间,从而提供持续的治疗效果。