Targeting xenobiotic receptors PXR and CAR in human diseases.
Targeting xenobiotic receptors PXR and CAR in human diseases.
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DOI：
10.1016/j.drudis.2014.11.011
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发表时间：
2015-05
影响因子：
7.4
通讯作者：
Chen T
中科院分区：
文献类型：
--
作者：
Banerjee M;Robbins D;Chen T
孕烷X受体（PXR）和组成型雄甾烷受体（CAR）等核受体是异生素受体，不仅调节药物代谢和处置，还调节多种人类疾病，如癌症、糖尿病、炎症性疾病、代谢疾病和肝脏疾病，表明PXR和CAR是药物发现的有前途的靶点。因此，迫切需要发现和开发针对这些 PXR 和/或 CAR 介导的人类疾病相关途径的小分子，以用于相关的治疗应用。本综述提出了在各种人类疾病的背景下单独或同时靶向 PXR 和 CAR 的方法，同时考虑到 PXR 和 CAR 之间的结构差异。
Nuclear receptors such as the pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are xenobiotic receptors regulating not only drug metabolism and disposition but also various human diseases such as cancer, diabetes, inflammatory disease, metabolic disease and liver diseases, suggesting that PXR and CAR are promising targets for drug discovery. Consequently, there is an urgent need to discover and develop small molecules that target these PXR- and/or CAR-mediated human-disease-related pathways for relevant therapeutic applications. This review proposes approaches to target PXR and CAR, either individually or simultaneously, in the context of various human diseases, taking into consideration the structural differences between PXR and CAR.