摘要
背景:人血清白蛋白(HSA)是血浆中最丰富的蛋白质,是一种单体多结构域大分子,具有至少9个内源性和外源性配体结合位点。 HSA具有出色的配体结合能力,可作为许多化合物(包括大多数酸性药物)的储库和载体。 因此,HSA有可能影响药物的药代动力学和药效学。 目的:在本综述中,将详细分析和讨论药物与HSA多个位点结合的结构决定因素。 此外,分析和讨论了对支持药物识别,递送和功效的变构和竞争机制的见解。 结论:由于多种因素可调节药物与HSA的结合(例如,同时给药竞争相同结合位点的药物,配体与变构偶联的裂隙结合,遗传遗传疾病和翻译后修饰),配体与HSA的结合至关重要,不仅在生理条件下,而且在药物治疗管理上。
关键词: 人血清白蛋白,药物载体,药物识别,结构基础,药物结合的变构调节,药物结合的竞争性调节。
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