A novel hirudin derivative inhibiting thrombin without bleeding for subcutaneous injection
作者: Bing ZhaoYanling ZhangYinong HuangJinchao YuYaran LiQi WangYixin MaHou-yan SongMin YuWei Mo
作者单位: 1Wei Mo, Key Laboratory of Metabolism and Molecular Medicine, Ministry of Education, Fudan University, Tel.: +86 21 54237440, Fax: +86 21 64033738, 238# P.O. Box, 138 Yixueyan Rd., Shanghai, 200032 , P. R. China, E-mail: weimo1025@shmu.edu.cn
刊名: Thromb Haemost, 2017, Vol.117 (1), pp.44-56
来源数据库: Schattauer GmbH
DOI: 10.1160/TH16-05-0416
关键词: Thrombinr-RGD-hirudinthrombosissubcutaneous injectiondirect thrombin inhibitor peptide (DTIP)
原始语种摘要: Currently, anticoagulants would be used to prevent thrombosis. Thrombin is an effector enzyme for haemostasis and thrombosis. We designed a direct thrombin inhibitor peptide (DTIP) using molecular simulation and homology modelling and demonstrated that the C-terminus of DTIP interacts with exosite I, and N-terminus with the activity site of thrombin, respectively. DTIP interfered with thrombin-mediated coagulation in human, rat and mouse plasma (n=10 per group) and blocked clotting in human whole blood in vitro. When administered subcutaneously, DTIP showed potent and dose-dependent extension of aPTT, PT, TT and CT in rats (n=10 per group). The antithrombotic dose of DTIP induced significantly less bleeding than bivalirudin determined by transecting distal tail assay in rats. Furthermore,...
全文获取路径: Schattauer 出版社 
影响因子:6.094 (2012)

  • thrombin 凝血酶
  • subcutaneous 皮下的
  • antithrombotic 抗血栓形成的
  • inhibiting 抑制
  • thrombosis 血栓形成
  • hirudin 水蛭素
  • novel 长篇小说
  • injection 贯入
  • pulmonary 肺的
  • increased 增加