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    • 1. 发明申请
    • ANALOGUES OF AN ANTI-THROMBIN POLYPEPTIDE AND PROCESS FOR THEIR PREPARATION
    • 抗凝血多肽的模拟物及其制备方法
    • WO1995003409A1
    • 1995-02-02
    • PCT/EP1994001979
    • 1994-06-17
    • FARMITALIA CARLO ERBA S.R.L.
    • FARMITALIA CARLO ERBA S.R.L.SCACHERI, EmanuelaVISCO, CarloMOLINARI, AntonioGERNA, MarcoBOLIS, Giorgio
    • C12N15/15
    • C07K14/005A61K38/00C07K14/815C07K2319/02C12N2760/20222
    • The present invention relates to analogues of anti-thrombin polypeptides and to a process for their preparation. The analogues have been obtained by a C-terminal modification of anti-thrombin polypeptides isolated from the leech Hirudinaria manillensis and are characterized by an improved biological activity in comparison to the polypeptides from which they are derived. The analogues of the invention may be prepared by: 1) isolating the anti-thrombin polypeptide from the tissue or secretions of the leech Hirudinaria manillensis and 2) subsequently modifying the C-terminal end of such polypeptide. Alternatively, the analogues may also be synthetized by recombinant DNA methods. According to this latter aspect, the invention provides DNA sequences, expression vectors and host cell lines for the recombinant preparation of the analogues. The analogues of the invention find a useful application in the treatment of venous thrombosis, vascular shunt occlusion and thrombin-induced disseminated intravascular coagulation.
    • 本发明涉及抗凝血酶多肽的类似物及其制备方法。 类似物已经通过从水蛭Hirudinaria manillensis分离的抗凝血酶多肽的C末端修饰获得,并且与从其衍生的多肽相比具有改善的生物学活性。 本发明的类似物可以通过以下方法制备:1)从水蛭水蛭属的组织或分泌物中分离抗凝血酶多肽,和2)随后修饰该多肽的C-末端。 或者,类似物也可以通过重组DNA方法合成。 根据后一方面,本发明提供用于重组制备类似物的DNA序列,表达载体和宿主细胞系。 本发明的类似物在治疗静脉血栓形成,血管分流闭塞和凝血酶诱导的弥散性血管内凝血方面发现有用。