华法林与α1-酸性糖蛋白（血清类黏蛋白）结合的pH依赖性
pH-dependence of warfarin binding to alpha 1-acid glycoprotein (orosomucoid).
作者信息
Urien S, Brée F, Testa B, Tillement J P
机构信息
INSERM, Paris, France.
出版信息
Biochem J. 1993 Feb 1;289 ( Pt 3)(Pt 3):767-70. doi: 10.1042/bj2890767.
Abstract
The binding of warfarin to alpha 1-acid glycoprotein (AAG) was found to increase with decreasing pH. The u.v.-visible difference spectra generated upon binding to AAG at pH 5.0 or 7.4 showed warfarin to bind as the anion. Warfarin-binding data were satisfactorily fitted to a model that incorporates the effect of pH and discriminates the association constants of the non-protonated and protonated binding site of the protein. It was shown that AAG-binding site in the protonated form had a markedly higher affinity for warfarin than the non-protonated form, with a pK value of 7.7 +/- 0.1, which is likely to be a histidine residue. Among other possible interactions, it is suggested that ligand binding to AAG involves a reinforced hydrogen bond.
摘要
发现华法林与α1-酸性糖蛋白（AAG）的结合随着pH值降低而增加。在pH 5.0或7.4下与AAG结合时产生的紫外可见差示光谱表明，华法林以阴离子形式结合。华法林结合数据令人满意地拟合到一个模型中，该模型纳入了pH值的影响，并区分了蛋白质非质子化和质子化结合位点的缔合常数。结果表明，质子化形式的AAG结合位点对华法林的亲和力明显高于非质子化形式，其pK值为7.7±0.1，这可能是一个组氨酸残基。在其他可能的相互作用中，有人提出配体与AAG的结合涉及增强的氢键。
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