纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | HTR1D |
Uniprot No | P28221 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-38aa |
氨基酸序列 | MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALK |
预测分子量 | 19.5 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HTR1D重组蛋白的3篇参考文献,按文献名称、作者和摘要内容概括整理:
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1. **文献名称**: *"Cloning and pharmacological characterization of the human 5-HT1D receptor"*
**作者**: Branchek TA, et al.
**摘要**: 该研究首次报道了人源HTR1D受体的基因克隆,并在哺乳动物细胞中重组表达。通过药理学分析发现,HTR1D与5-HT1B受体具有高度同源性,但对特定激动剂(如舒马普坦)的亲和力存在差异,提示其在偏头痛治疗中的潜在作用靶点。
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2. **文献名称**: *"Functional characterization of the recombinant human 5-HT1D receptor in mammalian cell lines"*
**作者**: Adham N, et al.
**摘要**: 作者在HEK293细胞中表达了重组HTR1D蛋白,并通过cAMP抑制实验验证其功能。研究表明,HTR1D通过Gi/o蛋白偶联信号通路介导细胞内信号传导,并揭示了其与配体结合的特异性及跨膜结构域的关键作用。
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3. **文献名称**: *"5-HT1D receptor antagonists inhibit cAMP production in transfected cells: evidence for constitutive receptor activity"*
**作者**: Pauwels PJ, Palmier C
**摘要**: 该文献利用重组HTR1D蛋白模型,发现某些拮抗剂可抑制基础状态下的cAMP水平,表明HTR1D存在组成性激活现象。这一发现为开发靶向该受体的反向激动剂提供了理论依据。
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4. **文献名称**: *"Pharmacological comparison of human and guinea pig 5-HT1D receptors expressed in recombinant systems"*
**作者**: Zgombick JM, et al.
**摘要**: 研究对比了人源与豚鼠HTR1D重组蛋白在昆虫细胞中的表达及药理学特性,揭示了物种间配体选择性和信号转导效率的差异,强调跨物种研究对药物开发的参考意义。
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以上文献聚焦于HTR1D的克隆、表达、信号机制及药理学特性研究,覆盖基础功能探索与潜在治疗应用。
**Background of HTR1D Recombinant Protein**
The 5-hydroxytryptamine receptor 1D (HTR1D), also known as 5-HT1D, is a G protein-coupled receptor (GPCR) that binds serotonin (5-hydroxytryptamine, 5-HT), a neurotransmitter regulating mood, cognition, and physiological processes. HTR1D is primarily expressed in the central nervous system (CNS), particularly in the basal ganglia, cortex, and hippocampus, as well as in peripheral tissues like blood vessels. It modulates neurotransmitter release by inhibiting adenylyl cyclase activity via Gi/o protein coupling, reducing intracellular cAMP levels.
Recombinant HTR1D protein is engineered in vitro using expression systems (e.g., mammalian, insect, or bacterial cells) to produce purified, functional receptor proteins for research. This involves cloning the HTR1D gene into a vector, transfecting host cells, and optimizing conditions to ensure proper folding, post-translational modifications, and ligand-binding activity. Mammalian systems like HEK293 or CHO cells are preferred for generating receptors with native-like structures.
HTR1D is studied for its role in neurological and vascular disorders. It is a target for migraine therapies, as triptans (e.g., sumatriptan) selectively activate 5-HT1B/1D receptors to constrict cranial blood vessels and inhibit pain signaling. Recombinant HTR1D enables structural studies (e.g., cryo-EM), ligand screening, and mechanistic insights into receptor dimerization, signaling pathways, and disease-linked mutations. Challenges include maintaining receptor stability during purification and ensuring compatibility with functional assays.
Overall, recombinant HTR1D is a critical tool for advancing serotonin receptor biology and developing therapeutics for migraines, anxiety, and depression.
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