Department of Pharmaceutical Sciences, St. Jude Children's Research Hospital, Memphis, Tennessee (J.D.S); Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland (P.W.S); and Department of Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim, Ridgefield, Connecticut (D.J.T.).
Drug Metab Dispos. 2014 Apr;42(4):541-5. doi: 10.1124/dmd.114.057539.
The significance of transporters in the disposition, metabolism, and elimination of drugs is well recognized. One gap in our knowledge is a comprehensive understanding of how drug transporters change functionality (their amount and activity) in response to disease and how disease and its inevitable pathology change transporter expression. In this issue of Drug Metabolism and Disposition a series of review and primary research articles are presented to highlight the importance of transporters in toxicity and disease. Because of the central role of the liver in drug metabolism, many of the articles in this theme issue focus on transporters in the liver and how pathology or alterations in physiology affects transporter expression. The contributing authors have also considered the role of transporters in drug interactions as well as drug-induced liver injury. Noninvasive approaches to assessing transporter function in vivo are also described. Several articles highlight important issues in oncology where toxicity must be balanced against efficacy. In total, this theme issue will provide a stepping-stone to future studies that will establish a more comprehensive understanding of transporters in disease.
药物转运体在药物的处置、代谢和消除中具有重要作用，这一点已得到广泛认可。目前我们的知识仍存在一个空白，即尚不完全清楚药物转运体如何针对疾病改变其功能（数量和活性），也不清楚疾病及其必然的病理变化如何改变转运体的表达。本期《药物代谢与处置》杂志发表了一系列综述和原始研究文章，重点强调了转运体在毒性和疾病中的重要性。由于肝脏在药物代谢中起着核心作用，本主题中的许多文章都集中于肝脏中的转运体，以及病理变化或生理学改变如何影响转运体的表达。撰稿人还考虑了转运体在药物相互作用以及药物性肝损伤中的作用。本文还描述了评估体内转运体功能的非侵入性方法。有几篇文章重点介绍了肿瘤学中的重要问题，其中毒性必须与疗效相平衡。总的来说，本期主题将为未来的研究提供一个垫脚石，以更全面地了解疾病中的转运体。
