CAJ | 학술논문

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 간우시일충이용쌍련RNA분자특이적침묵파기인표체적기술，목전이엄범용우기출생물의학연구。작위일충고선택성화유효적기인조공수단，저일기술야이용우림상질병적치료연구화약물전운체적연구。약물전운체시일류세포막단백，재약물적흡수、분포화배설중발휘중요작용。전운체공능적억제혹결실장개변약물적청제화약대동역학，도치약효강저혹독성증가。인차，재신약연발이급약물림상응용중，연구약물전운체재약물과막전운、조직분포、배설청제화약-약상호작용중적작용，대우약물적유효안전사용，구유중요의의。 RNA간우기술재약물전운체개도적약물전운화약-약상호작용연구방면，구유명현적우세。본문대근년래RNA간우기술재약물전운체연구중적응용진행종술，중점천술저일기술재약물전운체개도적종류내약、약물체내전운、청제화상호작용연구중적응용，위약물전운체적공능화조절연구제공삼고。
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.