Department of Pharmaceutical Analysis and Drug Metabolism, Zhejiang University, Hangzhou, Zhejiang 310058, China.
Curr Drug Metab. 2013 Feb;14(2):253-64.
Membrane transporters play a significant role in drug absorption, distribution and excretion, and they consequently affect the pharmacokinetics, efficacy and safety of a drug. Under certain circumstances, such as pathological processes or exposure to certain substances, the expression of drug transporters is modified in cells. Change in transporter expression and function may affect cellular drug disposition resulting in different drug responses. This raises a number of questions such as which drugs are likely to modulate the expression of drug transporters, what factors support this process, and which transporters are influenced in a particular situation. In this paper, we summarize recent findings to find an answer to these questions. Particularly, we present an overview of the transcription factors involved in the regulation of a given drug transporter, the signaling transduction pathways that contribute to drug transporter gene expression, and xenobiotics and endobiotics that initiate the processes.
膜转运蛋白在药物的吸收、分布和排泄中起着重要作用，因此影响药物的药代动力学、疗效和安全性。在某些情况下，如病理过程或暴露于某些物质，细胞中的药物转运蛋白表达会发生改变。转运蛋白表达和功能的改变可能会影响细胞内药物的处置，从而导致不同的药物反应。这就提出了一系列问题，例如哪些药物可能会调节药物转运蛋白的表达，支持这一过程的因素有哪些，以及在特定情况下哪些转运蛋白会受到影响。本文总结了最近的研究结果，以期回答这些问题。特别是，我们概述了参与特定药物转运蛋白调节的转录因子、参与药物转运蛋白基因表达的信号转导途径，以及启动这些过程的外源性和内源性物质。
