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血清白蛋白、脂质与药物结合

Serum Albumin, Lipid and Drug Binding.

作者信息

Nishi Koji, Yamasaki Keishi, Otagiri Masaki

机构信息

Faculty of Pharmaceutical Sciences, Sojo University, Ikeda 4-22-1, Nishi-Ku, Kumamoto, 860-0082, Japan.

DDS Research Institute, Sojo University, Ikeda 4-22-1, Nishi-Ku, Kumamoto, 860-0082, Japan.

出版信息

Subcell Biochem. 2020;94:383-397. doi: 10.1007/978-3-030-41769-7_15.

Abstract

Albumin is widely conserved from vertebrates to invertebrates, and nature of mammalian albumins permit them to bind various endogenous ligands and drugs in the blood. It is known that at least two major ligand binding sites are present on the albumin molecule, which are referred to as Site I and Site II. These binding sites are thought to be almost completely conserved among mammals, even though the degree of binding to these sites are different depending on the physical and chemical properties of drugs and differences in the microenvironment in the binding pockets. In addition, the binding sites for medium and long-chain fatty acids are also well conserved among mammals, and it is considered that there are at least seven binding sites, including Site I and Site II. These bindings properties of albumin in the blood are also widely known to be important for transporting drugs and fatty acids to various tissues. It can therefore be concluded that albumin is one of the most important serum proteins for various ligands, and information on human albumin can be very useful in predicting the ligand binding properties of the albumin of other vertebrates.

摘要

从脊椎动物到无脊椎动物,白蛋白都广泛存在,哺乳动物白蛋白的特性使其能够结合血液中的各种内源性配体和药物。已知白蛋白分子上至少存在两个主要的配体结合位点,分别称为位点I和位点II。尽管由于药物的物理化学性质以及结合口袋微环境的差异,药物与这些位点的结合程度有所不同,但这些结合位点在哺乳动物中被认为几乎是完全保守的。此外,中链和长链脂肪酸的结合位点在哺乳动物中也高度保守,并且认为至少有七个结合位点,包括位点I和位点II。白蛋白在血液中的这些结合特性对于将药物和脂肪酸运输到各种组织也非常重要。因此可以得出结论,白蛋白是各种配体最重要的血清蛋白之一,关于人类白蛋白的信息对于预测其他脊椎动物白蛋白的配体结合特性可能非常有用。

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