The binding of benzopyranes to human serum albumin.: A structure-affinity study

被引:9
作者
Ferrer, JM [1 ]
Leiton, MJ [1 ]
Zatón, AML [1 ]
机构
[1] Univ Basque Country, Fac Farm, Dept Bioquim & Biol Mol, Vitoria, Spain
来源
JOURNAL OF PROTEIN CHEMISTRY | 1998年 / 17卷 / 02期
关键词
albumin-ligand binding; benzopyrane binding; human serum albumin; anticoagulant drugs;
D O I
10.1023/A:1022575315391
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The binding of several benzopyranes to serum albumin was studied by equilibrium dialysis at pH 7.4 in a 67 mM sodium phosphate buffer at 37 degrees C. The equilibrium data were analyzed using a computer program for curve fitting. The binding isotherm for warfarin, 4-hydroxycoumarin, 4-chromanol, coumarin, 3-acetylcoumarin, and benzoic acid can be described by two stoichiometric dissociation constants. Elimination of the 4-hydroxyl group in the coumarin chemical structures decreases the binding affinity of the compounds on the primary binding site of serum albumin, with 4-chromanol the smallest ligand which binds to seroalbumin with high affinity. Thus, the affinity of 4-benzopyranol and the 4-hydroxybenzopyranones greater than that of benzopyranones. On the other hand, elimination of the 2-oxo group in the benzopyranone chemical structures decreases affinity for the secondary binding site.
引用
收藏
页码:115 / 119
页数:5
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