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国际病理 2009, 29(2) 160-164 DOI:
ISSN: 0412-1961 CN: 21-1139/TG |
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| 综述 |
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有机阳离子转运体OCT1的遗传药理学研究进展 |
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苑晋艳综述 周宏灏审校 |
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中南大学临床药理研究所 长沙 410008 |
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摘要：
为了排泄外源性物质和体内代谢产物，人体的肝脏、肾脏和肠道上广泛分布有各种转运体。其中有机阳离子转运体(organic cation transporters, OCTs)介导了一些药物、毒物和内源性化合物等一系列有机阳离子的转运。OCTs家族的第一成员OCT1在许多外源性药物的吸收、分布和排泄中发挥着重要的作用。OCT1存在许多基因多态性，有些多态性与其转运活性密切相关。此外，OCT1的转运活性可以被蛋白激酶C（protein kinase C,PKC）和蛋白激酶A（protein kinase A,PKA）所增强，这样介导了许多底物药物之间以及底物药物和PKC, PKA激活剂或抑制剂之间的相互作用。本文就OCT1的生理和遗传药理作用进行了综述。 |
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关键词：
有机阳离子转运体
基因多态性
药代动力学
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Pharmacogenetical functions of polyspecific organic cation transporter 1 |
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YUAN Jinyan,ZHOU Honghao
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Institute of Clinical Pharmacology, Central South University, Changsha 410008, China
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Abstract:
To eliminate environmental toxins and metabolic products, the body is equipped with kinds of transporters which are generally exist in liver, kidney, and intestine. The polyspecific organic cation transporters (OCTs) mediate the facilitated transport of a variety of structurally diverse organic cations, including many drugs, toxins, and endogenous compounds. In this review, we focus on its first identified member OCT1. Several genetic variations have been found in the human solute carrier(SLC)22A1 gene, which encodes OCT1, and many of these variations reduced its transport activity. It has been demonstrated that the organic cation transport by rOCT1 is stimulated by protein kinase C(PKC),protein kinase A(PKA). These may mediate drug-drug interaction between the inhibitors or activators of PKC or PKA and substrate-drugs of OCT1.This article will review the physical and pharmacogenetical functions of OCT1. |
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Keywords:
organic cation transporter
single nucleotide polymorphisms
pharmacokinetic
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收稿日期 2008-10-06 修回日期 2009-02-25 网络版发布日期 |
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DOI: |
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基金项目:
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通讯作者: 周宏灏 |
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