Review Article

核受体对ABC转运蛋白的调节:生理学,病理学和药理学方面

卷 26, 期 7, 2019

页: [1079 - 1112] 页: 34

弟呕挨: 10.2174/0929867324666170920141707

价格: $65

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摘要

ABC转运蛋白是介导内源和异生素外排的膜蛋白。转运蛋白表达不是静态的,而是受到动态调节,旨在响应内部环境的变化,从而维持稳态条件。核受体是配体调节的转录因子,其在各激动剂的细胞内浓度变化时被激活,并与ABC转运蛋白的启动子内的响应元件结合,从而调节它们的表达,从而调节它们的活性。本综述汇编了根据犯罪者化合物分类的核受体调节转运蛋白调节的信息以及调节产生的生物效应。激素受体的调节参与维持内分泌体内平衡,并且还可以在激素水平改变的情况下导致其他底物的外流改变。异生生物受体在限制潜在有害化合物的积累方面起着关键作用。此外,它们经常被治疗剂激活使它们成为介导药物 - 药物相互作用和癌症多药耐药性的常见分子元素。最后,脂质和类视黄醇受体通常由内源性分子激活,从而感知代谢变化并诱导ABC转运蛋白以抵消潜在的改变。此外,轴核受体-ABC转运蛋白构成了治疗癌症,动脉粥样硬化和血脂异常等几种疾病状态的有希望的治疗靶标。在目前的工作中,我们总结了关于核受体调节剂的药理学潜力的可用信息,并讨论了它们在临床实践中的适用性。

关键词: ABC转运蛋白,药物转运蛋白,核受体,药物相互作用,激素受体,Pglycoprotein,多药耐药相关蛋白,孕烷x受体。

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[http://dx.doi.org/10.1002/mnfr.201700055]

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