| 纯度 | >90%SDS-PAGE. |
| 种属 | Human |
| 靶点 | GPBAR1 |
| Uniprot No | Q8TDU6 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 1-330aa |
| 氨基酸序列 | MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLAGLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQPPGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGAAAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPYVATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQGLWGRASRDSPGPSIAYHPSSQSSVDLDLN |
| 预测分子量 | 36.8 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GPBAR1(TGR5)重组蛋白的3篇参考文献及其摘要概括：
1. **《Recombinant Human GPBAR1/TGR5 Characterization and Its Role in Bile Acid Signaling》**
*作者：Thomas et al. (2016)*
**摘要**：本研究成功在大肠杆菌中表达了重组人源GPBAR1蛋白，并优化了其纯化条件。通过体外功能实验证实，重组GPBAR1能够响应胆汁酸配体(如鹅去氧胆酸)激活cAMP信号通路，为后续药物筛选提供了工具。
2. **《Structural Insights into TGR5 Activation by Bile Acids Using a Thermally Stabilized Recombinant Receptor》**
*作者：Li et al. (2018)*
**摘要**：作者通过基因工程技术构建了热稳定性增强的GPBAR1重组蛋白，并利用冷冻电镜解析其与胆汁酸复合物的三维结构。该研究揭示了配体结合口袋的关键氨基酸残基，解释了受体激活的分子机制。
3. **《Expression and Functional Analysis of Recombinant GPBAR1 in Inflammatory Bowel Disease Models》**
*作者：Wang et al. (2020)*
**摘要**：研究在哺乳动物细胞中表达了功能性GPBAR1重组蛋白，并发现其激活可抑制巨噬细胞炎症因子(如TNF-α)的释放。结果提示GPBAR1重组蛋白在炎症性肠病治疗中具有潜在应用价值。
(注：上述文献为示例，实际引用需根据具体论文调整。建议通过PubMed或Web of Science以关键词“GPBAR1 recombinant”或“TGR5 expression”检索最新研究。)
GPBAR1 (G Protein-Bile Acid Activated Receptor 1), also known as TGR5. is a member of the G protein-coupled receptor (GPCR) family, first identified in 2002. It is activated by bile acids, particularly secondary bile acids like lithocholic acid (LCA) and its conjugated forms. Structurally, GPBAR1 features seven transmembrane domains characteristic of GPCRs and is expressed in various tissues, including the liver, intestine, gallbladder, immune cells, and adipose tissue, highlighting its role in systemic metabolic and immune regulation.
Functionally, GPBAR1 modulates energy homeostasis, glucose metabolism, and bile acid synthesis. Upon activation, it triggers intracellular signaling pathways (e.g., cAMP/PKA, MAPK) that influence enteroendocrine hormone secretion (e.g., GLP-1), promoting insulin sensitivity and mitochondrial energy expenditure. It also exerts anti-inflammatory effects by suppressing NF-κB signaling, linking it to inflammatory bowel disease and metabolic disorders. GPBAR1's involvement in cholesterol metabolism and bile acid circulation further connects it to liver diseases, such as cholestasis and non-alcoholic steatohepatitis (NASH).
Recombinant GPBAR1 protein, produced via mammalian or insect expression systems with tags (e.g., His, FLAG), retains native receptor conformation and activity. It is critical for in vitro studies, enabling ligand binding assays, receptor-ligand interaction analysis, and high-throughput drug screening. Structural studies using recombinant GPBAR1 have advanced the design of synthetic agonists/antagonists targeting metabolic syndromes, diabetes, and liver disorders. Its role in gut-liver axis communication and immune modulation also positions it as a therapeutic candidate for obesity-related inflammation and gastrointestinal pathologies. Overall, GPBAR1 recombinant tools are indispensable for deciphering its pathophysiology and developing precision therapies.
×
