2002年4月1日 · PXR is now widely accepted as the principal transcriptional regulator of CYP3A induction by xenobiotics. The constitutive androstane receptor (CAR) regulates the expression of CYP2B, which has a...

针对cyp酶诱导评估，我们可以提供pxr/ahr核受体激活实验和肝细胞诱导模型的服务，肝细胞诱导模型可以覆盖cyp3a4、 cyp2b6、cyp1a2以及cyp2c8、2c9和2c19亚型，提供包含mrna和酶活的数据，赋能客户的药物研发。

2024年5月14日 · PXR is a nuclear receptor that can be activated by diverse compounds to elevate metabolism, negatively impacting drug efficacy and safety. This presents a barrier to drug development because...

The pregnane X receptor (PXR) regulates expression of proteins responsible for all three phases required for the detoxification mechanism, which include CYP450 enzymes, phase II enzymes, and multidrug efflux pumps. Therefore, PXR is a prominent receptor that is responsible for xenobiotic excretion and drug–drug interactions.

摘要：目的 从孕烷x 受体(pxr)对药物代谢途径的调控入手，在代谢性药物相互作用、pxr 在cyp3a4 调控中的作用 及其调控机制等方面作分析和阐述。 方法 结合近年来国内外相关文献进行评述。

2010年3月19日 · In this study, we investigated the role of nuclear receptor binding to PXR response elements in CYP3A4, as a potential non-genetic mechanism contributing to interindividual variability of induction. By in vitro DNA binding experiments, we showed that several nuclear receptors bind efficiently to the proximal promoter ER6 and distal xenobiotic ...

2011年8月1日 · Pregnane X receptor (PXR), constitutive androstane receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors

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.

2001年6月14日 · The human nuclear pregnane X receptor (hPXR) activates cytochrome P450-3A expression in response to a wide variety of xenobiotics and plays a critical role in mediating dangerous drug-drug interact...

Pregnane X receptor (PXR, NR112) is a xenobiotic receptor whose primary function is to regulate the expression of drug-metabolizing enzymes (DMEs) and drug transporters. Drug-induced PXR activation and subsequent enzyme and transporter induction has been proposed to be an important mechanism for the drug-drug interactions.