Hepatocyte Hopping of OATP1B Substrates Contributes to Efficient Hepatic Detoxification
Hepatocyte Hopping of OATP1B Substrates Contributes to Efficient Hepatic Detoxification
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DOI：
10.1038/clpt.2012.143
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发表时间：
2012-11-01
影响因子：
6.7
通讯作者：
Schinkel, A. H.
中科院分区：
文献类型：
--
作者：
Iusuf, D.;van de Steeg, E.;Schinkel, A. H.
人有机阴离子转运多肽 (OATP) 1B1 和 OATP1B3 是存在于肝细胞基底外侧（正弦）膜中的主要药物摄取转运蛋白。由于其广泛的底物特异性，它们对许多阴离子药物的肝脏清除有重大影响，并且还影响疏水性甚至阳离子药物和药物缀合物的清除。最近的研究阐明了这些转运蛋白的几种生理和药理功能，以及它们通过“肝细胞跳跃”对肝脏最佳和灵活解毒的潜在贡献。
Human organic anion-transporting polypeptides (OATP) 1B1 and OATP1B3 are major drug uptake transporters present in the basolateral (sinusoidal) membrane of hepatocytes. Owing to their broad substrate specificity, they have a major impact on the hepatic clearance of numerous anionic drugs and also affect the clearance of hydrophobic and even cationic drugs and drug conjugates. Recent studies have clarified several physiologic and pharmacologic functions of these transporters, as well as their potential contributions to optimal and flexible detoxification in the liver by means of "hepatocyte hopping."