纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | NR1I2 |
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 | 69.8 kDa |
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. |
以下是关于NR1I2(PXR)重组蛋白的3篇参考文献,包含文献名称、作者及摘要概括:
1. **《Identification of a nuclear receptor for bile acids》**
*作者:Makishima M, et al.*
摘要:该研究报道了NR1I2(PXR)作为胆汁酸核受体的功能,利用重组蛋白技术证实PXR可被胆汁酸激活,调控药物代谢酶CYP3A4的表达,揭示了其在胆汁酸代谢中的作用机制。
2. **《Crystal structure of the pregnane X receptor-ecdysoone receptor ligand binding domain heterodimer with a selective modulator》**
*作者:Chrencik JE, et al.*
摘要:通过重组表达PXR与RXR的配体结合域,解析了其异源二聚体晶体结构,揭示了配体选择性调控的分子基础,为靶向PXR的药物设计提供了结构依据。
3. **《The human nuclear xenobiotic receptor PXR: genetic polymorphisms, alternative isoforms, and regulation by drugs》**
*作者:Lamba JK, et al.*
摘要:利用重组PXR蛋白研究其遗传多态性及剪接变体对药物响应的影响,发现不同异构体在配体结合和转录激活能力上的差异,解释了人群中药效差异的分子机制。
4. **《The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity》**
*作者:Xie W, et al.*
摘要:通过重组人源PXR蛋白实验,证明其作为石胆酸传感器的功能,能够通过诱导解毒酶表达缓解胆汁酸诱导的肝毒性,阐明PXR在肝脏保护中的关键作用。
这些研究均涉及NR1I2重组蛋白的表达与功能分析,涵盖结构解析、配体互作及代谢调控等领域。
**Background of NR1I2 Recombinant Protein**
Nuclear receptor subfamily 1 group I member 2 (NR1I2), commonly known as the pregnane X receptor (PXR), is a ligand-activated transcription factor belonging to the nuclear receptor superfamily. It plays a central role in regulating the expression of genes involved in xenobiotic detoxification and drug metabolism, including cytochrome P450 enzymes (e.g., CYP3A4), drug transporters (e.g., P-glycoprotein), and phase II conjugation enzymes. PXR is primarily expressed in the liver and intestine, where it senses lipophilic xenobiotics, such as pharmaceuticals, environmental toxins, and endogenous bile acids, and coordinates adaptive transcriptional responses to mitigate their toxic effects.
Recombinant NR1I2 protein is engineered for in vitro studies to elucidate its molecular interactions, ligand-binding properties, and regulatory mechanisms. Structurally, it contains a DNA-binding domain (DBD) for target gene recognition and a ligand-binding domain (LBD) that undergoes conformational changes upon agonist or antagonist binding. This protein is widely used in drug discovery to screen compounds for PXR activation or inhibition, which helps predict drug-drug interactions and assess potential toxicity.
The recombinant form is typically produced in expression systems like *E. coli* or mammalian cells, often fused with tags (e.g., His-tag) for purification and detection. Studies using recombinant NR1I2 have advanced understanding of its role in diseases, including cholestasis, inflammatory bowel disease, and cancer chemoresistance. Additionally, it serves as a tool to explore species-specific ligand responses, as PXR ligand preferences vary significantly between humans and preclinical models. Overall, NR1I2 recombinant protein is indispensable for dissecting the molecular basis of xenobiotic metabolism and developing safer therapeutics.
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