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外周型苯二氮䓬受体与原卟啉IX二氨基酸衍生物的相互作用。

Interactions of peripheral-type benzodiazepine receptor with diamino acid derivatives of protoporphyrin IX.

作者信息

Bombalska Aneta, Graczyk Alfreda

机构信息

Optoelectronic Institute, Military University of Technology, Gen. Sylwestra Kaliskiego 2 str., 00-908 Warsaw, Poland.

出版信息

J Photochem Photobiol B. 2009 Feb 9;94(2):138-42. doi: 10.1016/j.jphotobiol.2008.11.001. Epub 2008 Nov 14.

Abstract

The aim of this study was to examine and determine binding affinities of the peripheral benzodiazepine receptor (PBR) with diamino acid derivatives of protoporphyrin IX with general structure PP(AA)(2) in a function of environmental pH changes. Fluorescence intensity was used as a measure of protein association constant. Decrease in protein fluorescence, after titration with increasing concentration of porphyrins, gave evidence of interactions between PBR and examined ligands. Experimental data were fitted to theoretical curves, assuming different models of interactions. All examined ligands were best fitted to weak binding model. Increase in environmental acidity resulted in changes in association constants. For all examined derivatives association constants were at least twice higher in pH 5.5 as compared to pH 7.4 and 6.5.

摘要

本研究的目的是研究并确定外周苯二氮䓬受体(PBR)与具有通式PP(AA)(2)的原卟啉IX二氨基酸衍生物在环境pH变化时的结合亲和力。荧光强度被用作蛋白质结合常数的度量。用浓度不断增加的卟啉进行滴定后,蛋白质荧光强度降低,这证明了PBR与所研究配体之间存在相互作用。假设不同的相互作用模型,将实验数据拟合到理论曲线。所有研究的配体都最适合弱结合模型。环境酸度的增加导致结合常数发生变化。对于所有研究的衍生物,在pH 5.5时的结合常数比在pH 7.4和6.5时至少高出两倍。

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