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Fibrin crosslinking inhibitors and / or transglutaminases

机译:纤维蛋白交联抑制剂和/或转谷氨酰胺酶

摘要

B FIBRIN AND / OR TRANSGLUTAMINASE BINDING INHIBITORS D Inhibitors that can be obtained from tissues or secretions of leeches typically of the order Rhychobdellida have the following terminal sequence: NH ~ 2 ~ -Lys-Leu-Leu-Pro-Cys -Lys-Glu-Y-His-Gln-Gly-Ile-Pro-Asn-Pro-Arg, where Y represents any amino acid sequence; or a salt, derivative or bioprecursor of the pharmaceutically acceptable sequence, or an analog or homologue thereof. Due to their extreme potency in the nanomolar range, inhibitors can be used to treat various diseases where protein cross-linking is important. The inhibitors can be used in the treatment of Crohn's disease, tumor implantation, arteriosclerosis, trombic microangiopathy, fibrous skin growth, acne, scarring, glomerulonephritis, cataracts or infection with microfilarial nematodes. In particular, inhibitors can be used to reduce vessel stability so that they are more subject to lysis by thrombolytic agents.
机译:纤维蛋白和/或转谷氨酰胺酶结合抑制剂可以从组织或水分泌物中获得的抑制剂通常具有Rhychobdellida顺序,其末端序列如下: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;或其药学上可接受的序列的盐,衍生物或生物前体,或其类似物或同系物。由于其在纳摩尔范围内的极强效价,抑制剂可用于治疗蛋白质交联很重要的各种疾病。该抑制剂可用于治疗克罗恩氏病,肿瘤植入,动脉硬化,菱形微血管病,皮肤纤维生长,痤疮,疤痕,肾小球肾炎,白内障或微丝线虫感染。特别地,可以使用抑制剂来降低血管的稳定性,从而使它们更易于被溶栓剂溶解。

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