Zatón A M, Ferrer J M, Ruiz de Gordoa J C, Marquínez M A
Departamento de Bioqumica y Biología Molecular, Facultad de Farmacia,Universidad del Pas Vasco, Vitoria-Gasteiz, Spain.
Chem Biol Interact. 1995 Jul 14;97(2):169-74. doi: 10.1016/0009-2797(95)03613-q.
It is known that binding site I on human serum albumin (HSA) consists of a zone of two overlapping regions: the specific binding region represented by warfarin binding and the specific binding region represented by azapropazone and phenylbutazone binding. In this paper binding parameters to defatted HSA and to HSA with fatty acids (molar ratio of fatty acid/HSA = 4) were compared. High-affinity binding sites for warfarin, 4-chromanol, 4-hydroxycoumarin, coumarin, 3-acetylcoumarin and phenylbutazone (759,549 M-1 > Ka > 67,024 M-1) constitute binding site I on HSA. In this binding area defatted HSA can bind two molecules of warfarin, but the presence of fatty acids diminish the binding capacity of warfarin to HSA (2 > n > 1).
已知人血清白蛋白（HSA）上的结合位点I由两个重叠区域组成：以华法林结合为代表的特异性结合区域和以阿扎丙宗及保泰松结合为代表的特异性结合区域。本文比较了去脂HSA和脂肪酸（脂肪酸/HSA摩尔比 = 4）存在时HSA的结合参数。华法林、4-色满醇、4-羟基香豆素、香豆素、3-乙酰香豆素和保泰松的高亲和力结合位点（759,549 M-1 > Ka > 67,024 M-1）构成了HSA上的结合位点I。在该结合区域，去脂HSA可结合两分子华法林，但脂肪酸的存在会降低华法林与HSA的结合能力（2 > n > 1）。
