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Recombinant Human PXR protein

  • 中文名: 孕烷X受体(PXR)重组蛋白
  • 别    名: PXR;PXR;Nuclear receptor subfamily 1 group I member 2
货号: PA1000-8810
Price: ¥询价
数量:
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产品详情

纯度>90%SDS-PAGE.
种属Human
靶点PXR
Uniprot No O75469
内毒素< 0.01EU/μg
表达宿主E.coli
表达区间1-434aa
氨基酸序列MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEGCKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEERRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSSGCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLLPHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWECGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHRVVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPFATPLMQELFGITGS
预测分子量 69.8kDa
蛋白标签His tag N-Terminus
缓冲液PBS, pH7.4, containing 0.01% SKL, 1mM DTT, 5% Trehalose and Proclin300.
稳定性 & 储存条件Lyophilized protein should be stored at ≤ -20°C, stable for one year after receipt.
Reconstituted protein solution can be stored at 2-8°C for 2-7 days.
Aliquots of reconstituted samples are stable at ≤ -20°C for 3 months.
复溶Always centrifuge tubes before opening.Do not mix by vortex or pipetting.
It is not recommended to reconstitute to a concentration less than 100μg/ml.
Dissolve the lyophilized protein in distilled water.
Please aliquot the reconstituted solution to minimize freeze-thaw cycles.

参考文献

以下是关于PXR(孕烷X受体)重组蛋白的3篇代表性文献的简要信息:

1. **"The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism"**

*作者:Kliewer SA, Goodwin B, Willson TM*

摘要:综述了PXR作为核受体调控外源性物质代谢的分子机制,重点讨论了重组PXR蛋白在体外研究中对药物代谢酶(如CYP3A4)的转录调控作用。

2. **"Humanized xenobiotic response in mice expressing nuclear receptor SXR"**

*作者:Xie W, Barwick JL, Downes M, et al.*

摘要:通过构建表达人源化PXR(SXR)重组蛋白的小鼠模型,揭示了PXR介导的物种特异性药物应答机制及其在解毒通路中的核心作用。

3. **"Crystal structure of the pregnane X receptor-estradiol complex"**

*作者:Watkins RE, Wisely GB, Moore LB, et al.*

摘要:报道了重组人PXR蛋白与雌激素配体的共结晶结构,阐明了其配体结合域的结构特征及多配体结合能力,为药物相互作用研究提供结构基础。

注:以上文献均发表于2000-2003年间(Science, PNAS等期刊),是早期揭示PXR生物学功能的经典研究。如需近年研究或特定应用方向文献,建议补充说明需求。

背景信息

**Background of PXR Recombinant Protein**

The pregnane X receptor (PXR), also known as the steroid and xenobiotic receptor (SXR), is a nuclear receptor that plays a central role in regulating the detoxification and elimination of xenobiotics, including drugs, environmental toxins, and bile acids. Discovered in the late 1990s, PXR is primarily expressed in the liver and intestine, where it functions as a ligand-activated transcription factor. Upon binding to diverse ligands—such as prescription drugs, herbal compounds, or endogenous metabolites—PXR forms a heterodimer with the retinoid X receptor (RXR) and activates the transcription of genes encoding cytochrome P450 enzymes (e.g., CYP3A4), drug transporters, and phase II metabolic enzymes. This adaptive response enhances detoxification but also contributes to drug-drug interactions and interindividual variability in drug efficacy.

Recombinant PXR protein, produced via heterologous expression systems (e.g., *E. coli*, insect, or mammalian cells*)*, retains the functional domains necessary for ligand binding, DNA interaction, and co-regulator recruitment. Its production enables *in vitro* studies to characterize PXR-ligand interactions, screen for activators/inhibitors, and investigate structural mechanisms of receptor activation. Tagged versions (e.g., His-tag or GST-tag) facilitate purification and use in assays like electrophoretic mobility shift assays (EMSAs) or fluorescence polarization.

Research leveraging recombinant PXR has advanced drug development by identifying compounds that modulate PXR activity, thereby predicting metabolic interactions or toxicity. It also aids in studying polymorphisms affecting PXR function and exploring its roles beyond xenobiotic metabolism, such as in inflammation, cancer, and energy homeostasis. Despite challenges in maintaining receptor stability and ligand promiscuity, recombinant PXR remains a critical tool for mechanistic and translational studies in pharmacology and toxicology.

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