Gao Chun-Ying, Chen Xiao-Yan, Zhong Da-Fang
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Yao Xue Xue Bao. 2012 May;47(5):565-72.
Liver is regarded as one of the most important organs for drug clearance in the body, which mediates both the metabolism and biliary excretion of drugs. Transporters are a class of functional membrane proteins and control the movement of substances into or out of cells. Transporters, which are extensively expressed in the liver, play important roles in the drug hepatic disposition by regulating the uptake of drugs from blood into hepatocytes or the efflux of drugs and their metabolites into bile. In this review, the localization, functions and substrate selectivity of the major transporters in the liver will be summarized, and the impacts of these transporters on drug hepatic disposition, the potential drug-drug interactions as well as their genetic polymorphisms will also be reviewed.
肝脏被视为体内药物清除的最重要器官之一，它介导药物的代谢和胆汁排泄。转运体是一类功能性膜蛋白，控制物质进出细胞。转运体在肝脏中广泛表达，通过调节药物从血液进入肝细胞的摄取或药物及其代谢产物进入胆汁的外排，在药物肝脏处置中发挥重要作用。在本综述中，将总结肝脏中主要转运体的定位、功能和底物选择性，还将综述这些转运体对药物肝脏处置的影响、潜在的药物-药物相互作用及其基因多态性。
