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Recombinant Human NR1H4 protein

  • 中文名: 胆汁酸受体(NR1H4)重组蛋白
  • 别    名: NR1H4;BAR;FXR;HRR1;Bile acid receptor
货号: PA2000-3285
Price: ¥询价
数量:
大包装询价

产品详情

纯度>90%SDS-PAGE.
种属Human
靶点NR1H4
Uniprot No Q96RI1
内毒素< 0.01EU/μg
表达宿主E.coli
表达区间 1-486aa
氨基酸序列MVMQFQGLENPIQISPHCSCTPSGFFMEMMSMKPAKGVLTEQVAGPLGQNLEVEPYSQYSNVQFPQVQPQISSSSYYSNLGFYPQQPEEWYSPGIYELRRMPAETLYQGETEVAEMPVTKKPRMGASAGRIKGDELCVVCGDRASGYHYNALTCEGCKGFFRRSITKNAVYKCKNGGNCVMDMYMRRKCQECRLRKCKEMGMLAECMYTGLLTEIQCKSKRLRKNVKQHADQTVNEDSEGRDLRQVTSTTKSCREKTELTPDQQTLLHFIMDSYNKQRMPQEITNKILKEEFSAEENFLILTEMATNHVQVLVEFTKKLPGFQTLDHEDQIALLKGSAVEAMFLRSAEIFNKKLPSGHSDLLEERIRNSGISDEYITPMFSFYKSIGELKMTQEEYALLTAIVILSPDRQYIKDREAVEKLQEPLLDVLQKLCKIHQPENPQHFACLLGRLTELRTFNHHHAEMLMSWRVNDHKFTPLLCEIWDVQ
预测分子量 56 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.

参考文献

以下是关于NR1H4(FXR)重组蛋白的3篇参考文献的简要整理:

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1. **文献名称**:*"Structural insights into the molecular mechanism of the ligand-induced activation of the farnesoid X receptor"*

**作者**:Mi LZ, Devarakonda S, Harp JM, et al.

**摘要内容**:该研究通过表达并纯化重组人源FXR配体结合域(LBD),解析了其与激动剂结合的晶体结构,揭示了配体诱导的受体构象变化机制,为靶向FXR的药物设计提供了结构基础。

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2. **文献名称**:*"Recombinant FXR ligand-binding domain expression and characterization in bile acid-mediated transcriptional regulation"*

**作者**:Downes M, Verdecia MA, Roecker AJ, et al.

**摘要内容**:作者利用大肠杆菌系统表达了重组FXR蛋白的LBD,并验证其与胆汁酸(如CDCA)的结合能力,证明其通过招募共激活因子调控下游基因(如SHP)的转录活性。

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3. **文献名称**:*"Development of a fluorescence polarization assay for the identification of FXR antagonists using recombinant protein"*

**作者**:Zhou J, Liu Y, Zhuang S.

**摘要内容**:研究通过重组表达FXR蛋白,建立基于荧光偏振的高通量筛选体系,成功筛选出新型FXR拮抗剂,为代谢性疾病治疗药物开发提供了实验平台。

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以上文献均聚焦于NR1H4(FXR)重组蛋白的表达、结构功能研究及药物开发应用。如需具体出版年份或期刊信息,可进一步补充关键词检索。

背景信息

NR1H4. also known as farnesoid X receptor (FXR), is a nuclear receptor encoded by the NR1H4 gene. It functions as a ligand-activated transcription factor regulating bile acid, lipid, and glucose homeostasis. Primarily expressed in the liver, intestine, and kidneys, FXR is activated by endogenous bile acids such as chenodeoxycholic acid (CDCA). Upon activation, it forms heterodimers with retinoid X receptor (RXR) and binds to specific DNA response elements, modulating target genes like BSEP (bile salt export pump), SHP (small heterodimer partner), and FGF19. which collectively maintain metabolic balance.

Recombinant NR1H4 protein refers to the engineered form of FXR produced in vitro using expression systems like *E. coli* or mammalian cells. This purified protein retains functional domains, including the ligand-binding domain (LBD) and DNA-binding domain (DBD), enabling studies on receptor-ligand interactions and transcriptional regulation mechanisms. Its production often involves affinity tags (e.g., His-tag) for efficient purification.

Research on recombinant NR1H4 has advanced understanding of FXR's role in cholestasis, non-alcoholic fatty liver disease (NAFLD), diabetes, and atherosclerosis. It serves as a critical tool for drug discovery, facilitating high-throughput screening of FXR agonists/antagonists, such as obeticholic acid, a clinically approved FXR agonist for primary biliary cholangitis. Structural studies using recombinant protein have also elucidated mechanisms of ligand selectivity and co-regulator recruitment. Additionally, it aids in investigating cross-talk between FXR and other signaling pathways, including inflammation and fibrosis. This recombinant protein is vital for both basic research and therapeutic development targeting metabolic disorders.

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