| 纯度 | >90%SDS-PAGE. |
| 种属 | Human |
| 靶点 | HCRTR1 |
| Uniprot No | O43613 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 1-46aa |
| 氨基酸序列 | MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYE |
| 预测分子量 | 21.4 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HCRTR1重组蛋白的3篇参考文献及其摘要内容：
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1. **文献名称**：*Structure and ligand-binding mechanism of the human OX1 orexin receptor*
**作者**：Yin, J., Babaoglu, K., Brautigam, C.A., et al.
**摘要**：该研究通过X射线晶体学解析了人源HCRTR1(OX1受体)的晶体结构，揭示了其与拮抗剂结合的分子机制，阐明了受体与配体相互作用的特异性位点，为靶向药物设计提供了结构基础。
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2. **文献名称**：*Orexin receptors: pharmacology and therapeutic opportunities*
**作者**：Sakurai, T., Mieda, M.
**摘要**：综述了HCRTR1和HCRTR2的生理功能及药理学特性，重点讨论了重组HCRTR1蛋白在药物开发中的应用，包括其在失眠、成瘾等疾病中的潜在治疗靶点作用。
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3. **文献名称**：*Mutational analysis of the human orexin 1 receptor: roles of conserved amino acids in receptor activation and G-protein coupling*
**作者**：Malherbe, P., Borroni, E., Pinard, E., et al.
**摘要**：通过定点突变和重组HCRTR1蛋白表达，研究了受体关键氨基酸残基在信号转导和G蛋白偶联中的作用，揭示了其激活机制及与下游效应分子的相互作用。
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4. **文献名称**：*Development of a high-throughput screening assay for the human orexin-1 receptor using fluorescence polarization*
**作者**：Thompson, M.D., Percy, M.E., Xiong, Y.
**摘要**：利用重组HCRTR1蛋白建立了一种基于荧光偏振的高通量筛选方法，用于快速筛选和评估小分子配体的结合活性，为抗失眠药物开发提供高效工具。
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以上文献涵盖了HCRTR1的结构解析、功能研究、药物开发及实验方法学方向，均为该领域的代表性研究。
The hypocretin receptor type 1 (HCRTR1), also known as orexin receptor type 1. is a G protein-coupled receptor (GPCR) that binds neuropeptides hypocretin-1 and hypocretin-2 (orexin-A and orexin-B). It is primarily expressed in the central nervous system, particularly in regions regulating arousal, energy homeostasis, and stress responses. HCRTR1 activation triggers intracellular signaling cascades, primarily via Gq proteins, influencing neuronal excitability and neurotransmitter release.
Recombinant HCRTR1 protein is engineered for research and therapeutic applications. Produced through recombinant DNA technology in systems like mammalian cells or bacteria, it retains structural and functional properties of the native receptor. This allows studies on ligand-receptor interactions, signal transduction mechanisms, and drug screening. Recombinant HCRTR1 is critical in exploring pathologies linked to orexin signaling dysregulation, such as narcolepsy, insomnia, and metabolic disorders. It also aids in developing antagonists (e.g., for insomnia) or agonists targeting sleep-wake disorders.
Mutations or altered expression of HCRTR1 have been implicated in neurological and psychiatric conditions, including addiction and anxiety. Research using recombinant protein has clarified its role in modulating reward pathways and stress adaptation. Additionally, structural studies of recombinant HCRTR1. often combined with cryo-EM or X-ray crystallography, provide insights into receptor activation and guide rational drug design. Its applications extend to biomarker discovery and personalized medicine, particularly for disorders with orexin system involvement.
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