CILASTATIN (MK 0791) IS A POTENT AND SPECIFIC INHIBITOR OF THE RENAL LEUKOTRIENE-D4-DIPEPTIDASE
CILASTATIN (MK 0791) IS A POTENT AND SPECIFIC INHIBITOR OF THE RENAL LEUKOTRIENE-D4-DIPEPTIDASE
复制标题
DOI：
10.1016/0006-291x(85)91335-x
复制
发表时间：
1985-01-01
影响因子：
3.1
通讯作者：
KONIG, W
中科院分区：
文献类型：
--
作者：
KOLLER, M;RAULF, M;KONIG, W
西司他丁 (MK 0791)（一种已知的肾脱氢肽酶 I 抑制剂）强烈抑制肾组织二肽酶将白三烯 D4 代谢为白三烯 E4。与其他组织（肝、肺、血清、多形核粒细胞）的类似酶活性的比较揭示了西司他丁对肾酶的高度特异性，该肾酶被发现与微粒体部分相关。肾组织内西司他丁的最低可检测抑制浓度为8倍。 10-8 M。
The metabolism of leukotriene D4 to leukotriene E4 by a dipeptidase of kidney tissue is strongly inhibited by cilastatin (MK 0791) a known renal dehydropeptidase-I inhibitor. The comparison with similar enzyme activities from other tissues (liver, lung, serum, polymorphonuclear granulocytes) revealed a high specificity of cilastatin for the kidney enzyme which was found to be associated with the microsomal fraction. The lowest detectable inhibitory concentration of cilastatin within renal tissue was 8 .times. 10-8 M.