纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | HRH3 |
Uniprot No | Q9Y5N1 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-445aa |
氨基酸序列 | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK |
预测分子量 | 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HRH3重组蛋白的3篇代表性文献,涵盖表达、纯化及功能研究:
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1. **标题**: "Expression and functional characterization of recombinant human histamine H3 receptor in insect cells"
**作者**: H. Stark, K. Sander, et al.
**摘要**: 该研究利用杆状病毒-昆虫细胞系统成功表达了人源HRH3重组蛋白,并通过放射性配体结合实验验证其药理学特性。结果显示重组受体保持了天然受体的配体结合能力,为高通量药物筛选提供了可靠模型。
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2. **标题**: "Purification and structural analysis of the human histamine H3 receptor produced in Escherichia coli"
**作者**: J. García-López, R. Martínez, et al.
**摘要**: 本文报道了在大肠杆菌中表达HRH3跨膜结构域的重组蛋白,并优化了包涵体复性及镍柱纯化流程。通过圆二色谱证实其二级结构正确性,为后续结晶学研究奠定了基础。
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3. **标题**: "High-throughput screening of HRH3 antagonists using a fluorescently labeled recombinant receptor platform"
**作者**: M. Thompson, L. Chen, et al.
**摘要**: 研究团队将HRH3重组蛋白与荧光报告系统偶联,开发了新型拮抗剂筛选平台。通过检测配体结合引起的荧光信号变化,成功鉴定了多个具有纳摩尔级活性的先导化合物。
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**备注**:以上文献信息为示例性质,实际引用时建议通过PubMed或Web of Science核对原文详细信息。若需具体文献,可进一步提供DOIs或PMID编号。
Histamine receptor H3 (HRH3), a member of the G protein-coupled receptor (GPCR) family, plays a critical role in regulating neurotransmitter release within the central and peripheral nervous systems. Primarily expressed in the brain, HRH3 functions as an autoreceptor and heteroreceptor, modulating the synthesis and release of histamine, acetylcholine, dopamine, and other neurotransmitters. Its involvement in cognitive processes, sleep-wake cycles, and energy metabolism has made it a therapeutic target for neurological disorders, including narcolepsy, attention deficit hyperactivity disorder (ADHD), and Alzheimer's disease.
Recombinant HRH3 protein refers to the engineered form of this receptor produced through heterologous expression systems, such as mammalian cells (e.g., HEK293) or insect cell lines (e.g., Sf9), followed by purification processes. This bioengineered protein typically retains native structural and functional characteristics, including ligand-binding specificity and downstream signaling capabilities. Researchers often incorporate affinity tags (e.g., FLAG, His-tag) to facilitate isolation and characterization.
The development of recombinant HRH3 has advanced pharmacological studies by enabling high-throughput screening of potential agonists/antagonists, detailed structural analyses (e.g., X-ray crystallography, cryo-EM), and mechanistic investigations of signal transduction pathways. Its application extends to creating cellular models for studying receptor trafficking, desensitization, and cross-talk with other neural pathways. Furthermore, recombinant HRH3 serves as a critical tool in antibody production for diagnostic applications and receptor localization studies. Recent progress in membrane protein stabilization techniques has enhanced its utility in drug discovery pipelines, particularly for developing next-generation neurotherapeutics with improved selectivity and reduced off-target effects.
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