PXR、CAR和VDR是密切相关的核受体，在BA解毒和清除过程中发挥相似的作用。 虽然CAR没有任何已知的BA配体，但这三种核受体都能促进肝毒性LCA 的清除。 LCA激活的PXR和VDR增加了 CYP3A 和SULT的表达。 它们还促进了LCA输出蛋白OATP2和多药耐药蛋白3 (MRP3)的表达。 此外，PXR、CAR和VDR通过FGF15/FGF19途径抑制CYP7a1，有助于BA稳态。 2002 年 Maruyama 等首次报道了一种新的胆汁酸膜受体 TGR5，属于 G 蛋白偶联受体（GPCR）超家 …

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2023年3月4日 · pxr、car和vdr是密切相关的核受体，在ba解毒和清除过程中发挥相似的作用。虽然car没有任何已知的ba配体，但这三种核受体都能促进肝毒性lca 的清除。lca激活的pxr和vdr增加了cyp3a和sult的表达。它们还促进了lca输出蛋白oatp2和多药耐药蛋白3 (mrp3)的表达。

2021年6月1日 · PXR and CAR are xenobiotic receptors that regulate the expression of drug-metabolizing enzymes and transporters. PXR and CAR have equally important roles in governing the homeostasis of numerous endobiotics. PXR and CAR have overlapping yet distinct functions in liver physiology and pathophysiology.

孕烷X受体(pregnant X receptor,PXR)和组成型雄甾烷受体(constitutive androstane receptor,CAR)是核受体(nuclear receptors,NRs)超家族的重要成员,主要分布在肝脏和小肠等组织,经配体激活后可调控药物代谢酶及转运体的表达和活性,调节毒性物质的清除、解毒及代谢,保护机 …

2005年1月15日 · The liver X receptors α and β (LXRα/β, NR1H3/2) and the farnesoid X receptor (FXR, NR1H4) have several features in common with CAR, PXR, and VDR, other members of the NR1I subfamily: they are lipid-activated nuclear receptors, they bind their ligands with relative low affinity, often in the micromolar range and they heterodimerize with the ...

2016年6月3日 · 通过主要介绍核受体家族主要成员 PXR 、 CAR 、LXR 和 FXR 在糖异生、脂类代谢以及胆汁平衡中的调控作用，从而可能为糖脂代谢和胆汁平衡紊乱相关代谢性疾病的药物治疗提供新依据。

Taken together, these data demonstrate that both PXR and CAR, in addition to FXR, are important in controlling bile acid homeostasis, especially during cholestasis. Although FXR has not been directly linked to any human disease, its target genes have been implicated in several inherited cholestatic liver disorders.

2008年9月30日 · Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily of ligand-activated transcription factors. As a metabolic regulator, FXR plays key roles...

The farnesoid-x-receptor (FXR), the constitute-androstane-receptor (CAR) and the pregnane-x-receptor (PXR) are ligand regulated nuclear receptors highly expressed in the liver and intestine supervising essential steps in the metabolism of xeno and endo-biotics in entero-hepatic tissues.