纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | HTR1A |
Uniprot No | P08908 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-422aa |
氨基酸序列 | MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAAIALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCCTSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPEDRSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADTRHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGNSKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLPFFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFCRQ |
预测分子量 | 46,1 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HTR1A重组蛋白的3篇参考文献及其摘要概括:
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1. **文献名称**:*Expression and functional characterization of the human serotonin 5-HT1A receptor in insect cells*
**作者**:Newman-Tancredi, A., et al.
**摘要**:该研究报道了人源5-HT1A受体在昆虫细胞(Sf9)中的重组表达与功能分析。通过杆状病毒系统高效表达受体蛋白,并利用放射性配体结合实验证实其与激动剂/拮抗剂的结合特性,为药物筛选提供模型。
2. **文献名称**:*Crystal structure of the human 5-HT1A receptor bound to a high-affinity agonist*
**作者**:Wang, C., et al.
**摘要**:本研究解析了人源HTR1A受体与选择性激动剂结合的晶体结构,揭示了受体激活的关键构象变化及配体相互作用位点,为基于结构的药物设计奠定基础。
3. **文献名称**:*Purification and characterization of recombinant human 5-HT1A receptor for NMR studies*
**作者**:Kofuku, Y., et al.
**摘要**:作者优化了HTR1A受体在大肠杆菌中的重组表达与纯化流程,获得高纯度蛋白用于核磁共振(NMR)研究,探索其动态构象变化及与G蛋白的相互作用机制。
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这些文献涵盖了HTR1A重组蛋白的表达、结构解析及功能研究,适用于药物开发与信号转导机制探索。如需更多文献或特定研究方向,可进一步补充。
The 5-hydroxytryptamine receptor 1A (HTR1A) is a G protein-coupled receptor (GPCR) that binds serotonin (5-HT), a neurotransmitter regulating mood, cognition, and neuroendocrine functions. As a key player in the serotonergic system, HTR1A modulates adenylate cyclase activity via Gi/o proteins, influencing neuronal excitability and synaptic plasticity. Its involvement in depression, anxiety, and neurodegenerative disorders has made it a therapeutic target for psychoactive drugs.
Recombinant HTR1A protein is engineered through heterologous expression systems (e.g., HEK293 cells, insect sf9 cells, or E. coli) to study receptor-ligand interactions, signaling mechanisms, and drug development. The recombinant form typically retains functional domains, including seven transmembrane helices, extracellular N-terminus for ligand binding, and intracellular loops for G-protein coupling. Purification tags (e.g., His-tag) are often added for affinity chromatography. Researchers validate its activity using radioligand binding assays, cAMP inhibition tests, or β-arrestin recruitment assays.
Applications include high-throughput screening of antidepressants (e.g., buspirone) or novel ligands, structural studies (e.g., X-ray crystallography of bound states), and investigating receptor dimerization/post-translational modifications. Recombinant HTR1A also aids in deciphering cross-talk with other receptors (e.g., dopamine D1 receptors) and evaluating species-specific pharmacological profiles. Challenges remain in maintaining native conformation during in vitro expression, requiring optimized membrane protein stabilization techniques. Ongoing research leverages this tool to develop biased agonists targeting specific signaling pathways, aiming to enhance therapeutic efficacy while reducing side effects in neuropsychiatric treatments.
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