摘要
背景:人血清白蛋白(HSA)是人血清中最丰富的蛋白质。 它具有许多功能,其中之一是小疏水分子的运输,包括药物,毒素,营养素,激素和代谢物。 HSA具有与各种结构不同的化合物相互作用的能力。 当两种或多种化合物竞争结合到相同分子位点时,这种混杂的非特异性亲和力可导致由置换引起的浓度的突然变化。 目的:在定义给药方案时,考虑药物组合及其与HSA的结合是重要的,因为它可以直接影响药物的血液中游离,积极的浓度。 结论:在本文中,我们回顾了药物相互作用与HSA的位移潜力,可能发生的情况及其临床意义。 我们还提供设计减少与HSA结合的药物的指导方针。
关键词: 人血清白蛋白,药物置换,药代动力学相互作用,游离浓度,药物设计
Current Medicinal Chemistry
Title:Displacement of Drugs from Human Serum Albumin: From Molecular Interactions to Clinical Significance
Volume: 24 Issue: 18
关键词: 人血清白蛋白,药物置换,药代动力学相互作用,游离浓度,药物设计
摘要: Background: Human serum albumin (HSA) is the most abundant protein in human serum. It has numerous functions, one of which is transport of small hydrophobic molecules, including drugs, toxins, nutrients, hormones and metabolites. HSA has the ability to interact with a wide variety of structurally different compounds. This promiscuous, nonspecific affinity can lead to sudden changes in concentrations caused by displacement, when two or more compounds compete for binding to the same molecular site.
Objective: It is important to consider drug combinations and their binding to HSA when defining dosing regimens, as this can directly influence drug’s free, active concentration in blood. Conclusion: In present paper we review drug interactions with potential for displacement from HSA, situations in which they are likely to occur and their clinical significance. We also offer guidelines in designing drugs with decreased binding to HSA.Export Options
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Cite this article as:
Displacement of Drugs from Human Serum Albumin: From Molecular Interactions to Clinical Significance, Current Medicinal Chemistry 2017; 24 (18) . https://dx.doi.org/10.2174/0929867324666170202152134
DOI https://dx.doi.org/10.2174/0929867324666170202152134 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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