孕烷X受体:肝脏疾病的潜在药物靶标  

Pregnane X Receptor: a Potential Therapeutic Target for Liver Diseases

作　　者：辛瑜[1] 杨暄 奚涛[1] 熊晶[2] XIN Yu;YANG Xuan;XI Tao;XIONG Jing(School of Life Science and Technology,China Pharmaceutical University,Nanjing 210009,China;Department of Pharmacology,Nanjing Medical University,Nanjing 210029,China)

机构地区：[1]中国药科大学生命科学与技术学院,江苏南京210009 [2]南京医科大学基础医学院药理学系,江苏南京210029

出　　处：《药学进展》2018年第12期922-928,共7页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金(No.81302855);江苏省自然科学基金(No.BK2012446)

摘　　要：孕烷X受体(PXR)属于配体依赖性调控靶基因的核受体亚家族,激活后可调控多种药物代谢酶和转运体的表达,影响临床药物的疗效和耐药性。PXR通过调控肝脏中脂质和糖类物质的代谢,影响肝脏疾病的发生发展进程,可作为肝脏疾病药物筛选与疾病治疗的潜在药物靶标。深入了解PXR及其调控机制对于预测药物-药物相互作用、避免或减轻药物不良反应以及设计和研发以PXR为靶点的新型药物均具有十分重要的意义。对PXR在肝脏疾病中的调控作用及药物通过PXR干预肝脏疾病进程的研究进展进行概述。Pregnane X receptor(PXR), a member of the nuclear receptor subfamily of ligand-dependent regulatory target genes, regulates the expression of multiple drug metabolizing enzymes and transporters upon activation, thus affecting the efficacy and drug resistance of clinical medicines. PXR is involved in the pathogenesis and development liver diseases by regulating the metabolism of lipids and carbohydrates in the liver, emerging as a potential drug target for drug screening and treatment of liver diseases. The deep understanding of PXR and its regulatory mechanisms has great significance for predicting drug-drug interactions, avoiding or mitigating adverse drug reactions, designing and developing novel drugs targeting PXR. This article summarized the regulatory roles of PXR in liver diseases and the research progress in drug intervention for liver disease progression through PXR.

关 键 词：孕烷X受体 药物研发 药物代谢 肝脏疾病 

分 类 号：R966[医药卫生—药理学]