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Selective inhibitors of plasma kallikrein.

作者信息

Evans D M, Jones D M, Pitt G R, Sueiras-Diaz J, Horton J, Ashworth D, Olsson H, Szelke M

机构信息

Ferring Research Institute, University of Southampton Research Centre, Chilworth, UK.

出版信息

Immunopharmacology. 1996 May;32(1-3):115-6.

PMID:8796284
Abstract

Based on a tetrapeptide fragment [Pro387-Ser390] of HK we have developed a series of potent low molecular weight (5-600 Da) inhibitors of PK which are stable to the enzyme. These inhibitors show good selectivity for PK versus tissue kallikrein, thrombin and plasmin. Such inhibitors will help define the role of PK and kinins in human physiology and pathophysiology. They may also find clinical use in the treatment of diseases where kinins are important mediators.

摘要

相似文献

1
Selective inhibitors of plasma kallikrein.
Immunopharmacology. 1996 May;32(1-3):115-6.
2
Synthetic inhibitors of human tissue kallikrein.
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3
Development of selective inhibitors against plasma kallikrein.
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Synthesis of potent and selective inhibitors of human plasma kallikrein.人血浆激肽释放酶强效和选择性抑制剂的合成
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Highly selective synthetic inhibitors with regard to plasma-kallikrein activities.对血浆激肽释放酶活性具有高度选择性的合成抑制剂。
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7
Development of plasma kallikrein selective inhibitors.血浆激肽释放酶选择性抑制剂的研发。
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Synthetic inhibitors of tissue kallikrein: effects in vivo in a model of allergic inflammation.
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J Lab Clin Med. 1992 Jul;120(1):129-39.

引用本文的文献

1
Kallikrein inhibitors limit kinin B(2) antagonist-induced progression of oedematous to haemorrhagic pancreatitis in rats.激肽释放酶抑制剂可限制大鼠中缓激肽B(2)拮抗剂诱导的水肿性胰腺炎向出血性胰腺炎的进展。
Br J Pharmacol. 2008 Nov;155(6):865-74. doi: 10.1038/bjp.2008.321. Epub 2008 Aug 11.
2
Neutrophils and the kallikrein-kinin system in proteinase-activated receptor 4-mediated inflammation in rodents.蛋白酶激活受体4介导的啮齿动物炎症中的中性粒细胞与激肽释放酶-激肽系统
Br J Pharmacol. 2005 Nov;146(5):670-8. doi: 10.1038/sj.bjp.0706371.
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Involvement of tissue kallikrein but not plasma kallikrein in the development of symptoms mediated by endogenous kinins in acute pancreatitis in rats.
组织激肽释放酶而非血浆激肽释放酶参与大鼠急性胰腺炎内源性激肽介导的症状发展过程。
Br J Pharmacol. 2002 Nov;137(5):692-700. doi: 10.1038/sj.bjp.0704910.