药物转运体OAT2研究进展

有机阴离子转运体2(OAT2)属于有机阴离子转运体家族成员,主要分布于肝肾,介导肌酐、尿酸等内源性物质及多种外源性药物的跨膜转运。OAT2对外源性物质如药物的体内过程如吸收、分布、代谢和排泄过程起着重要作用。研究表明OAT2的表达与活性被药物、疾病、性别及基因多态性等多种因素影响,亦受到核受体等信号通路调控。故本文综述药物转运体OAT2的结构与分布、底物、调控机制、临床意义的研究进展,为OAT2可能介导药物相互作用及药物疗效预测提供参考。

Progress on drug transporter organic anion transporter 2

Organic anion transporter 2(OAT2), an important member of organic anion transporter family, is mainly localized on canalicular membrane of hepatocyte and the basolateral membrane of renal epithelium. OAT2 plays a key role in transmembrane transport of xenobiotic or endogenous substrates, and OAT2 governs drug pharmacokinetics such as absorption, distribution, metabolism and excretion. Expressions and activities of OAT2 are modulated by diseases, drugs, genders, gene polymorphisms and nuclear receptors. Therefore, this paper will review advances of drug transporter OAT2 in structure, distribution, substrates, regulating mechanisms and clinical significances.