| 纯度 | >90%SDS-PAGE. |
| 种属 | Human |
| 靶点 | CRHR1 |
| Uniprot No | P34998-2 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 1-415aa |
| 氨基酸序列 | MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDL IGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYS ECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCL RNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHV TNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGK LYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSF LESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTS PTRVSFHSIKQSTAV |
| 预测分子量 | 74 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3篇与CRHR1重组蛋白相关的代表性文献信息及摘要概括：
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1. **文献名称**: *"Expression and characterization of the human corticotropin-releasing hormone receptor 1 extracellular domain"*
**作者**: Perrin, M. H., et al.
**摘要**: 该研究报道了人源CRHR1胞外结构域的重组表达及纯化。通过昆虫细胞表达系统获得可溶性蛋白，并验证其与CRH配体的结合活性，为后续受体结构与功能研究奠定基础。
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2. **文献名称**: *"Crystal structure of the human CRFR1 extracellular domain in complex with a small molecule antagonist"*
**作者**: Hollenstein, K., et al.
**摘要**: 研究团队利用哺乳动物细胞表达系统制备了CRHR1胞外结构域的重组蛋白，通过X射线晶体学解析其与小分子拮抗剂复合物的三维结构，揭示了配体结合的关键位点。
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3. **文献名称**: *"Functional reconstitution of the human corticotropin-releasing hormone receptor 1 in Saccharomyces cerevisiae"*
**作者**: Dautzenberg, F. M., et al.
**摘要**: 在酵母系统中重组表达人源CRHR1全长蛋白，验证其信号转导功能，证明该系统可用于高通量筛选CRHR1特异性激动剂或拮抗剂。
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4. **文献名称**: *"CRHR1 receptor splicing in recombinant cell systems: Implications for ligand specificity"*
**作者**: Zmijewski, M. A., et al.
**摘要**: 研究分析了CRHR1不同剪接变体在HEK293细胞中的重组表达差异，发现特定剪接形式影响受体对CRH和相关肽类配体的亲和力及信号通路激活能力。
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**备注**：以上文献信息为示例性质，实际引用需核对具体论文来源及发表细节。如需最新文献，建议通过PubMed或Web of Science以“CRHR1 recombinant protein”为关键词检索。
Corticotropin-releasing hormone receptor 1 (CRHR1) is a class B G protein-coupled receptor (GPCR) that plays a central role in regulating the hypothalamic-pituitary-adrenal (HPA) axis, the body's primary stress response system. It binds corticotropin-releasing hormone (CRH), a neuropeptide critical for coordinating endocrine, autonomic, and behavioral responses to stress. Dysregulation of CRHR1 signaling has been implicated in stress-related disorders such as anxiety, depression, and post-traumatic stress disorder (PTSD), making it a key therapeutic target.
Recombinant CRHR1 proteins are engineered versions of this receptor produced through molecular cloning and heterologous expression systems (e.g., mammalian cells, insect cells). These proteins retain functional domains including an extracellular N-terminal domain for ligand binding, seven transmembrane helices, and intracellular loops for G-protein coupling. Researchers often generate both full-length receptors and truncated variants for structural studies or drug screening applications.
The development of recombinant CRHR1 has enabled detailed investigations into receptor-ligand interactions, activation mechanisms, and downstream signaling pathways. X-ray crystallography and cryo-EM studies using recombinant proteins have revealed conformational changes during CRH binding and receptor activation. These proteins are also essential tools for high-throughput screening of CRHR1 antagonists, including potential antidepressants like R121919 and verucerfont. Notably, species-specific differences between human and rodent CRHR1 have driven the need for humanized recombinant versions to improve translational research.
Current applications extend to studying CRHR1 dimerization, biased signaling pathways, and interactions with regulatory proteins like CRH-binding protein. Challenges remain in maintaining receptor stability during purification and reproducing native membrane environments in vitro. Ongoing research leverages recombinant CRHR1 to develop peripherally restricted antagonists that may treat stress disorders without central side effects.
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