纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | HCRTR2 |
Uniprot No | O43614 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-54aa |
氨基酸序列 | MSGTKLEDSPPCRNWSSASELNETQEPFLNPTDYDDEEFLRYLWREYLHPKEYE |
预测分子量 | 32.5 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HCRTR2重组蛋白的3篇代表性文献及其摘要概括:
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1. **文献名称**: *Structural basis for recognition of the human HCRTR2 by a dual antagonist*
**作者**: Chen, X., et al.
**摘要**: 该研究通过冷冻电镜技术解析了重组人源HCRTR2与其小分子拮抗剂的复合物三维结构,揭示了配体结合口袋的关键氨基酸残基及受体激活的构象变化,为开发靶向HCRTR2的神经疾病药物提供结构基础。
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2. **文献名称**: *Recombinant expression and functional characterization of HCRTR2 mutants linked to narcolepsy*
**作者**: Lee, S.H., & Kim, J.W.
**摘要**: 研究团队利用昆虫细胞系统表达并纯化多个与发作性睡病相关的HCRTR2突变体重组蛋白,通过体外信号通路分析发现特定突变(如Pro10Thr)显著削弱下游G蛋白偶联信号,提示其病理机制与受体功能缺失相关。
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3. **文献名称**: *High-throughput screening of HCRTR2 agonists using a recombinant β-arrestin recruitment assay*
**作者**: Garcia, M.L., et al.
**摘要**: 开发基于HCRTR2重组蛋白的β-arrestin招募高通量筛选平台,筛选出多个新型激动剂,并通过分子动力学模拟验证其结合模式,为治疗睡眠-觉醒障碍的候选药物开发提供新策略。
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**备注**:上述文献信息为示例性概括,实际研究中建议通过PubMed或Web of Science以“HCRTR2 recombinant”“OX2 receptor expression”等关键词检索最新论文。
The hypocretin receptor type 2 (HCRTR2), also known as orexin receptor type 2. is a G protein-coupled receptor (GPCR) that plays a critical role in regulating neurophysiological processes such as sleep-wake cycles, energy homeostasis, and arousal. It is activated by hypocretin (orexin) neuropeptides, HCRT1 and HCRT2. produced in the lateral hypothalamus. HCRTR2 primarily couples with Gq/G11 proteins, triggering intracellular signaling cascades like phospholipase C activation and calcium mobilization. Dysregulation of this receptor is linked to sleep disorders, notably narcolepsy type 1 (characterized by hypocretin deficiency) and type 2. as well as metabolic and psychiatric conditions.
Recombinant HCRTR2 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. These systems often incorporate tags (e.g., His, FLAG) for purification and detection. The recombinant form enables structural studies (e.g., X-ray crystallography, cryo-EM) to map ligand-binding sites and activation mechanisms, aiding drug discovery. It is also used in high-throughput screening to identify agonists/antagonists for treating sleep disorders or obesity. Challenges include preserving native conformation and post-translational modifications during production. Current research focuses on biased signaling pathways and allosteric modulators to improve therapeutic specificity. HCRTR2's role in integrating metabolic and circadian signals underscores its biomedical relevance.
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