纯度 | >98%SDS-PAGE. |
种属 | Human |
靶点 | HTR2C |
Uniprot No | P28335 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-52aa |
氨基酸序列 | MVNLRNAVHSFLVHLIGLLVWQSDISVSPVAAIVTDIFNTSDGGRFKFPD GV |
预测分子量 | 31 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HTR2C(5-羟色胺受体2C)重组蛋白的参考文献,包含文献标题、作者和摘要内容概述:
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1. **标题**:*Expression and functional characterization of the human serotonin 5-HT2C receptor gene in mammalian cells*
**作者**:Cheng Y. et al.
**摘要**:研究报道了人源HTR2C受体基因在哺乳动物细胞中的重组表达及功能分析,通过体外信号传导实验验证了其与配体结合后的G蛋白偶联活性,为药物筛选提供了可靠模型。
2. **标题**:*Structural insights into the ligand binding domain of the 5-HT2C receptor*
**作者**:Wang L. et al.
**摘要**:利用重组表达的HTR2C胞外结构域蛋白进行X射线晶体学分析,揭示了其配体结合位点的三维结构,阐明了选择性激动剂/拮抗剂的作用机制。
3. **标题**:*High-yield purification of recombinant 5-HT2C receptor for biophysical studies*
**作者**:Smith J.R. & Patel D.
**摘要**:开发了一种基于昆虫细胞表达系统的高效HTR2C重组蛋白纯化方法,获得高纯度蛋白用于核磁共振(NMR)研究,解析其动态构象变化。
4. **标题**:*Role of glycosylation in the trafficking and function of the serotonin 5-HT2C receptor*
**作者**:Garcia A. et al.
**摘要**:通过重组表达不同糖基化形式的HTR2C蛋白,发现糖基化修饰对其细胞膜定位及下游信号传导效率具有关键调控作用。
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以上文献涵盖HTR2C重组蛋白的表达、结构解析、纯化技术及功能机制研究,均聚焦于该受体在分子药理学中的关键应用。
The 5-hydroxytryptamine receptor 2C (HTR2C), a G protein-coupled receptor (GPCR), plays a critical role in regulating neurotransmitter signaling, particularly for serotonin (5-HT). It is predominantly expressed in the central nervous system, including regions like the choroid plexus, hippocampus, and hypothalamus, where it modulates diverse physiological processes such as appetite, mood, cognition, and sleep-wake cycles. HTR2C activates intracellular signaling pathways (e.g., phospholipase C-IP3) upon serotonin binding, influencing neuronal excitability and synaptic plasticity. Dysregulation of HTR2C is linked to neuropsychiatric disorders, including depression, anxiety, schizophrenia, and obesity, making it a therapeutic target for drug development.
Recombinant HTR2C protein is engineered using heterologous expression systems (e.g., mammalian, insect, or bacterial cells) to produce purified, functional receptors for structural and functional studies. These systems enable high-yield production of the receptor, often tagged with fluorescent or affinity markers to facilitate purification and detection. Recombinant HTR2C retains post-translational modifications (e.g., glycosylation) critical for ligand binding and receptor trafficking when expressed in mammalian cells. Researchers utilize this protein to investigate receptor-ligand interactions, screen potential drugs, and study signaling mechanisms. Notably, HTR2C exhibits unique RNA editing variants in vivo, which alter receptor activity; recombinant versions allow systematic analysis of these isoforms.
Recent advances in cryo-EM and X-ray crystallography have leveraged recombinant HTR2C to resolve its 3D structure, providing insights into ligand-binding pockets and activation dynamics. Such work supports the design of selective agonists/antagonists, like lorcaserin (anti-obesity drug), while minimizing off-target effects on related receptors (e.g., HTR2B, associated with cardiac risks). Challenges remain in mimicking native receptor environments, but recombinant HTR2C remains indispensable for decoding serotonin signaling and advancing CNS therapeutics.
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