Uptake and efflux transporters for conjugates in human hepatocytes.

作者: Dietrich Keppler

DOI: 10.1016/S0076-6879(05)00029-7

关键词:

摘要: Conjugates of endogenous substances and xenobiotics, formed extrahepatically or inside hepatocytes, undergo vectorial transport into bile. Substances conjugated with glucuronate, sulfate, glutathione are substrates for organic anion uptake transporters in the basolateral (sinusoidal) membrane as well unidirectional ATP-driven conjugate efflux pump apical (canalicular) membrane, termed multidrug resistance protein 2 (MRP2; systematic name ABCC2). Localization pumps ABCC3 ABCC4 to human hepatocytes has provided insight molecular mechanisms from blood, exemplified by bilirubin glucuronosides mediated ABCC3. The cloning stable expression complementary DNAs encoding members ABCC subfamily have improved our understanding hepatobiliary elimination substrate specificity respect anionic conjugates. hepatocyte polarized cell lines, described this chapter, provides valuable tools vitro analysis general specifically conjugates various phase reactions.

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