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Inhibitors of fibrin cross-linking and/or transglutaminases

机译:纤维蛋白交联和/或转谷氨酰胺酶抑制剂

摘要

The inhibitors, obtainable from tissue or secretions of leeches typically of the order Rhynchobdellida, has the following terminal sequence: NH.sub.2 -Lys-Leu-Leu-Pro-Cys-Lys-Glu-Y-His-Gln-Gly- Ile-Pro- Asn-Pro-Arg- wherein Y represents any amino acid sequence; or a pharmaceutically acceptable salt, derivative or bioprecursor of said sequence, or an analogue or homologue thereof. Because of their extreme potency in the nanomolar range, they can be used to treat a number of diseases where protein cross-linking is important. They can be used for the treatment of Crohn's disease, tumor implantation, atherosclerosis, thrombotic microangiophathy, fibrous growths of the skin, acne, scar formation, membranous glomerulonephrits, cataracts, or infection with microfilarial nematodes. In particular, they can be used to reduce the stability of thrombi so that they are more susceptible to lysis by thrombolytic agents.
机译:可从通常为Rhynchobdellida阶的水or组织或分泌物中获得的抑制剂具有以下末端序列:NH 2 -Lys-Leu-Leu-Pro-Cys-Lys-Glu-Y-His-Gln-Gly- Ile-Pro-Asn-Pro-Arg-,其中Y代表任何氨基酸序列;或其序列的药学上可接受的盐,衍生物或生物前体,或其类似物或同系物。由于它们在纳摩尔范围内的极强效价,因此可用于治疗许多蛋白质交联很重要的疾病。它们可用于治疗克罗恩病,肿瘤植入,动脉粥样硬化,血栓性微血管吞噬,皮肤纤维生长,痤疮,疤痕形成,膜性肾小球肾炎,白内障或微丝线虫感染。特别地,它们可用于降低血栓的稳定性,从而使它们更易于被血栓溶解剂溶解。

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