RNA 干扰是一种利用双链RNA分子特异的沉默靶基因表达的技术，目前已广泛用于基础生物医学研究。作为一种高选择性和有效的基因调控手段，这一技术也已用于临床疾病的治疗研究和药物转运体的研究。药物转运体是一类细胞膜蛋白，在药物的吸收、分布和排泄中发挥重要作用。转运体功能的抑制或缺失将改变药物的清除和药代动力学，导致药效降低或毒性增加。因此，在新药研发以及药物临床应用中，研究药物转运体在药物跨膜转运、组织分布、排泄清除和药-药相互作用中的作用，对于药物的有效安全使用，具有重要意义。 RNA干扰技术在药物转运体介导的药物转运和药-药相互作用研究方面，具有明显的优势。本文对近年来RNA干扰技术在药物转运体研究中的应用进行综述，重点阐述这一技术在药物转运体介导的肿瘤耐药、药物体内转运、清除和相互作用研究中的应用，为药物转运体的功能和调节研究提供参考。%RNA interference ( RNAi) is a powerful technique that utilizes double-stranded RNA mole-cules to specifically knock down the expression of the targeted gene. The RNAi technique has a broad application to basic biomedical research. Thanks to its high selectivity and effectivity, this technique is also used clinically as a disease intervention and therapeutic method as well as in the research of drug transporters. Drug transporters are membrane proteins that play important roles in the absorption, distri-bution and elimination of a wide range of drugs. lnhibition or deletion of transporters may affect clearance and pharmacokinetics of drugs and lead to altered toxicity or therapeutic efficacy. Therefore, in drug development and clinical application, it has become critically important to characterize the roles of trans-porters in transmembrane transport, tissue distribution, clearance of drugs and drug-drug interactions. However, the diversity and complexity of transporters make it difficult to identify and confirm the role of transporters in drug transportation and drug-drug interactions using chemical inhibitors of transporters. RNAi is an excellent method in delineating their specific roles in drug distribution, elimination and drug-drug interactions. This article reviews recent studies using RNAi to silence gene expression of specific transporters and the application to the research of transporters mediated cancer resistance, drug disposition, clearance and drug-drug interactions.
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