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    • 2. 发明授权
    • Peptide fragments of tissue plasminogen activator
    • 组织纤溶酶原激活物的肽片段
    • US5039791A
    • 1991-08-13
    • US432256
    • 1989-11-06
    • Arthur J. WittwerMichael A. Sanzo
    • Arthur J. WittwerMichael A. Sanzo
    • A61K38/00C12N9/72
    • C12N9/6459C12Y304/21069A61K38/00
    • Novel peptide fragments of tissue plasminogen activator are described which have activity for inhibiting (a) the binding of tPA to human endothelial cells, and (b) the inactivation of tPA by plasminogen activator inhibitor-1 (PAI-1). Six peptides or peptide amides with these activities have the sequences, numbered according to the native protein:tPA (31-55),tPA (81-105),tPA (181-205),tPA (301-325),tPA (451-475, andtPA (531-555).It is hoped that small, synthesizeable molecules which prevent the inactivation of tPA by PAI-1 may provide a means for improving the efficacy of therapeutically administered tPA or for reducing the tendency of patients with elevated plasma PAI-1 concentrations to form fibrin clots.
    • 描述了组织纤溶酶原激活物的新型肽片段,其具有抑制(a)tPA与人内皮细胞结合的活性,和(b)通过纤溶酶原激活物抑制剂-1(PAI-1)灭活tPA。 具有这些活性的六种肽或肽酰胺具有根据天然蛋白质编号的序列:tPA(31-55),tPA(81-105),tPA(181-205),tPA(301-325),tPA(451 -475和tPA(531-555),希望通过PAI-1阻止tPA失活的小的合成分子可以提供治疗性给药tPA或降低患者倾向的方法 血浆PAI-1浓度形成纤维蛋白凝块。