| 纯度 | >90%SDS-PAGE. |
| 种属 | Human |
| 靶点 | EDNRA |
| Uniprot No | P25101-1 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 21-427aa |
| 氨基酸序列 | DNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRSSHKDSMN |
| 预测分子量 | 47.9 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. |
1. **《Structure of the human endothelin receptor A (EDNRA) in complex with endothelin-1》**
- 作者：Hirata, K. 等
- 摘要：通过X射线晶体学解析了EDNRA与内皮素-1结合的复合物结构，揭示了配体结合口袋的关键氨基酸残基及其相互作用机制，为靶向药物设计提供结构基础。
2. **《Functional characterization of recombinant EDNRA in vascular smooth muscle cells》**
- 作者：Sakamoto, A. 等
- 摘要：研究利用重组EDNRA蛋白在平滑肌细胞中验证其介导的钙信号通路和血管收缩功能，证实其在高血压相关病理中的潜在作用。
3. **《Pharmacological profiling of EDNRA mutants using recombinant protein expression systems》**
- 作者：Yanagisawa, M. 等
- 摘要：通过哺乳动物表达系统制备EDNRA突变体重组蛋白，分析不同突变对受体亲和力和信号转导的影响，揭示疾病相关基因变异的分子机制。
4. **《Targeting EDNRA in cancer-associated fibroblasts: A recombinant protein-based therapeutic strategy》**
- 作者：Kurihara, H. 等
- 摘要：基于重组EDNRA蛋白的体外实验和动物模型，证明抑制其活性可减少肿瘤微环境中纤维化的形成，为癌症治疗提供新思路。
**Background of EDNRA Recombinant Protein**
Endothelin Receptor Type A (EDNRA) is a G protein-coupled receptor (GPCR) that binds endothelin-1 (ET-1), a potent vasoconstrictor peptide involved in cardiovascular regulation, cell proliferation, and tissue remodeling. EDNRA is primarily expressed in vascular smooth muscle cells, where it mediates ET-1-induced vasoconstriction, and plays roles in pathophysiological processes such as hypertension, pulmonary arterial hypertension (PAH), and cancer progression. Dysregulation of EDNRA signaling is linked to fibrotic disorders, cardiovascular diseases, and tumor angiogenesis.
Recombinant EDNRA protein is engineered *in vitro* using expression systems (e.g., mammalian, insect, or bacterial cells) to produce functional receptor domains or full-length proteins for research and therapeutic applications. This protein retains ligand-binding activity and structural integrity, enabling studies on receptor-ligand interactions, downstream signaling pathways (e.g., Gq/11-mediated calcium mobilization), and drug screening. EDNRA is a key target for antagonist development; FDA-approved drugs like ambrisentan selectively block EDNRA to treat PAH by inhibiting vasoconstriction and vascular remodeling.
In cancer research, EDNRA overexpression in tumors (e.g., prostate, ovarian) correlates with aggressive phenotypes, making it a potential biomarker or therapeutic target. Recombinant EDNRA also aids in antibody production, structural biology studies (e.g., crystallography), and elucidating mechanisms of drug resistance. Challenges include maintaining receptor stability post-purification and mimicking native conformational states. Ongoing research focuses on optimizing EDNRA recombinant variants for high-throughput assays and personalized medicine approaches, emphasizing its dual role in cardiovascular and oncological therapeutics.
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