孕烷X受体(PXR)是一类配体依赖性的核受体亚家族,可感受外源物质,被多种药物激活。PXR可转录调控多种与药物代谢相关的药物代谢酶和药物转运体的表达,参与药物代谢调控。PXR转录活性的变化可改变药物在体内的代谢过程,继而诱发潜在药物不良反应,与药物药代动力学研究和临床药物治疗密切相关,并有潜力成为防治药物介导的肝损伤和逆转化疗药物耐药的新型药物靶标。综述了目前已发现的PXR翻译后修饰及其对PXR功能调控机制的研究进展。 Pregnane X receptor (PXR) is a ligand-dependent nuclear receptor subfamily, which can sense exogenous substances and is activated by various drugs. PXR transcriptional regulation of a variety of drug metabolism-related drug metabolism enzymes and drug transporter expression, involved in drug metabolism regulation. Changes in PXR transcriptional activity can alter the drug’s in vivo metabolism and subsequently induce potential adverse drug reactions that are closely linked to pharmacokinetic studies and clinical drug therapy and have the potential to become drug-mediated liver injury and reverse chemotherapeutic drugs Drug-resistant new drug target. The progress of PXR posttranslational modifications and their regulation of PXR function are reviewed.