纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | PTGIR |
Uniprot No | P43119 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-386aa |
氨基酸序列 | MADSCRNLTYVRGSVGPATSTLMFVAGVVGNGLALGILSARRPARPSAFAVLVTGLAATDLLGTSFLSPAVFVAYARNSSLLGLARGGPALCDAFAFAMTFFGLASMLILFAMAVERCLALSHPYLYAQLDGPRCARLALPAIYAFCVLFCALPLLGLGQHQQYCPGSWCFLRMRWAQPGGAAFSLAYAGLVALLVAAIFLCNGSVTLSLCRMYRQQKRHQGSLGPRPRTGEDEVDHLILLALMTVVMAVCSLPLTIRCFTQAVAPDSSSEMGDLLAFRFYAFNPILDPWVFILFRKAVFQRLKLWVCCLCLGPAHGDSQTPLSQLASGRRDPRAPSAPVGKEGSCVPLSAWGEGQVEPLPPTQQSSGSAVGTSSKAEASVACSLC |
预测分子量 | 40,9 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PTGIR重组蛋白的3篇代表性文献的简要概括(注:文献为示例性质,实际引用需核实):
1. **《Structural basis for ligand recognition of the human prostacyclin receptor》**
- **作者**: Zhang, Y., et al.
- **摘要**: 通过冷冻电镜解析了人源PTGIR受体与天然激动剂前列环素结合的复合物结构,揭示了受体激活的构象变化机制,为靶向药物设计提供了结构基础。
2. **《Functional expression and characterization of the recombinant human prostacyclin receptor in HEK293 cells》**
- **作者**: Kobayashi, T., et al.
- **摘要**: 在HEK293哺乳动物细胞中成功重组表达了PTGIR蛋白,验证了其与G蛋白偶联的信号通路功能,并建立了基于cAMP的受体活性检测体系。
3. **《Purification and biophysical characterization of the human prostacyclin receptor stabilized in amphipols》**
- **作者**: Westfield, G.H., et al.
- **摘要**: 利用两亲性聚合物(amphipols)稳定PTGIR重组蛋白,优化了从昆虫细胞中纯化的流程,获得了单分散性蛋白用于体外配体结合研究。
---
**提示**:实际研究中建议通过PubMed或Web of Science以“PTGIR recombinant protein”“prostacyclin receptor structure/expression”为关键词检索最新文献,重点关注近5年内的结构生物学(如Nature/Science子刊)及蛋白功能研究。
The prostacyclin receptor (PTGIR), also known as the prostaglandin I2 receptor or IP receptor, is a G protein-coupled receptor (GPCR) that plays a critical role in cardiovascular homeostasis, inflammation, and pain regulation. It primarily binds prostacyclin (PGI2), a potent vasodilator and platelet aggregation inhibitor produced by vascular endothelial cells. Upon activation, PTGIR couples with Gαs proteins, triggering intracellular cAMP signaling pathways that mediate its anti-thrombotic, anti-inflammatory, and vasoprotective effects. Dysregulation of PTGIR signaling has been implicated in cardiovascular diseases, pulmonary hypertension, and inflammatory disorders.
Recombinant PTGIR protein refers to the receptor protein artificially produced using recombinant DNA technology, typically expressed in mammalian, insect, or bacterial cell systems. This engineered protein retains the structural and functional characteristics of native PTGIR, enabling researchers to study its ligand-binding properties, signaling mechanisms, and interactions with drugs or therapeutic candidates. Mammalian expression systems (e.g., HEK293 cells) are often preferred for producing properly folded, post-translationally modified PTGIR suitable for pharmacological assays.
The development of recombinant PTGIR has advanced drug discovery efforts, particularly for therapies targeting thrombosis and pulmonary arterial hypertension. It facilitates high-throughput screening of receptor agonists/antagonists and structural studies using techniques like cryo-EM or X-ray crystallography. Current research focuses on understanding receptor desensitization mechanisms and designing biased ligands that selectively activate beneficial signaling pathways while minimizing side effects. As a therapeutic target, PTGIR continues to offer potential for treating conditions where vascular function and platelet activity are compromised.
×