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脂肪酸诱导人血清白蛋白N构象和B构象异质性的证据。

Evidence for the fatty acid-induced heterogeneity of the N and B conformations of human serum albumin.

作者信息

Dröge J H, Janssen L H, Wilting J

出版信息

Biochem Pharmacol. 1985 Sep 15;34(18):3299-304. doi: 10.1016/0006-2952(85)90349-1.

DOI:10.1016/0006-2952(85)90349-1
PMID:4038338
Abstract

The influence of oleic acid on the interaction between albumin and warfarin, oxyphenbutazone or diazepam has been studied by circular dichroism and equilibrium dialysis. The pH dependences of the molar ellipticity of the drug-albumin complexes and of the free fraction of drug are completely changed by the presence of oleic acid. This phenomenon is attributed to an oleic acid-induced conformational change in both the neutral (N) and the basic (B) conformation of albumin, a change to which the warfarin-oxyphenbutazone binding area and the diazepam binding site is sensitive. The oleic acid-induced conformational states of albumin, the so-called N* and B* conformations, show binding properties that are different from the binding properties of the N and B conformations.

摘要

通过圆二色性和平衡透析研究了油酸对白蛋白与华法林、奥沙普秦或地西泮之间相互作用的影响。油酸的存在完全改变了药物 - 白蛋白复合物的摩尔椭圆率和药物游离分数的pH依赖性。这种现象归因于油酸诱导的白蛋白中性(N)和碱性(B)构象的构象变化,华法林 - 奥沙普秦结合区域和地西泮结合位点对这种变化敏感。油酸诱导的白蛋白构象状态,即所谓的N和B构象,显示出与N和B构象的结合特性不同的结合特性。

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