Department of Surgery, Oncology and Gastroenterology, University of Padova, 35121 Padova, Italy.
Department of Pharmaceutical and Pharmacological Sciences, University of Padova, 35121 Padova, Italy.
Cells. 2021 Dec 27;11(1):61. doi: 10.3390/cells11010061.
Pregnane X receptor (PXR), a nuclear receptor known for modulating the transcription of drug metabolizing enzymes and transporters (DMETs), such as cytochrome P450 3A4 and P-glycoprotein, is functionally involved in chronic liver diseases of different etiologies. Furthermore, PXR activity relates to that of other NRs, such as constitutive androstane receptor (CAR), through a crosstalk that in turn orchestrates a complex network of responses. Thus, besides regulating DMETs, PXR signaling is involved in both liver damage progression and repair and in the neoplastic transition to hepatocellular carcinoma. We here summarize the present knowledge about PXR expression and function in chronic liver diseases characterized by different etiologies and clinical outcome, focusing on the molecular pathways involved in PXR activity. Although many molecular details of these finely tuned networks still need to be fully understood, we conclude that PXR and its modulation could represent a promising pharmacological target for the identification of novel therapeutical approaches to chronic liver diseases.
pregnane X 受体(PXR)是一种核受体,已知可调节药物代谢酶和转运体(DMETs)的转录,如细胞色素 P450 3A4 和 P-糖蛋白,其功能与不同病因的慢性肝脏疾病有关。此外,PXR 的活性与其他 NRs(如组成型雄烷受体(CAR))相关,通过串扰调节复杂的反应网络。因此,除了调节 DMETs 外,PXR 信号还参与肝损伤的进展和修复以及向肝细胞癌的肿瘤转化。我们在这里总结了 PXR 在具有不同病因和临床结局的慢性肝脏疾病中的表达和功能的现有知识,重点介绍了 PXR 活性涉及的分子途径。尽管这些精细调控网络的许多分子细节仍有待充分理解,但我们得出结论,PXR 及其调节可能是确定慢性肝脏疾病新治疗方法的有前途的药理学靶点。