HIGH-AFFINITY BINDING OF ETHACRYNIC-ACID IS MEDIATED BY THE 2 MOST IMPORTANT DRUG-BINDING SITES OF HUMAN-SERUM ALBUMIN
HIGH-AFFINITY BINDING OF ETHACRYNIC-ACID IS MEDIATED BY THE 2 MOST IMPORTANT DRUG-BINDING SITES OF HUMAN-SERUM ALBUMIN
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DOI：
10.1159/000138171
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发表时间：
1986-04-01
期刊：
影响因子：
3.1
通讯作者：
MULLER, WE
中科院分区：
文献类型：
--
作者：
FEHSKE, KJ;MULLER, WE
通过圆二色性和平衡透析测量来研究依他尼酸与人血清白蛋白的结合，使用天然人血清白蛋白和化学修饰的白蛋白衍生物，分别损害药物与吲哚和苯二氮卓结合位点或阿扎哌酮-华法林结合区域的特异性结合。所提供的数据表明，依他尼酸与人血清白蛋白的高亲和力结合是由这两个重要的药物结合位点介导的。因此，即使在相对较低的浓度下，依他尼酸也会从两个结合位点取代其他药物。
The binding of ethacrynic acid to human serum albumin was investigated by means of circular dichroism and equilibrium dialysis measurements, using native human serum albumin and albumin derivatives with chemical modifications impairing specifically drug binding to the indole and benzodiazepine binding site or the azapropazone-warfarin binding area, respectively. The data presented indicate that the high-affinity binding of ethacrynic acid to human serum albumin is mediated by these two important drug binding sites. Accordingly, even at relatively low concentrations ethacrynic acid displaces other drugs from both binding sites.