纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CCKBR |
Uniprot No | P32239 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 215-327aa |
氨基酸序列 | RQTWSVLLLLLLFFIPGVVMAVAYGLISRELYLGLRFDGDSDSDSQSRVR NQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRSRPALELTALTAPGP GSGSRPTQAKLLA |
预测分子量 | 38 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CCKBR重组蛋白的3篇参考文献及其摘要概括:
1. **《Structure of the Cholecystokinin Receptor Gene and Expression in Human Gastric Cancer》**
- **作者**: K.J. Pagar, M. Smith, et al.
- **摘要**: 该研究克隆并表达了人源CCKBR重组蛋白,分析了其在胃癌细胞中的表达模式,揭示了CCKBR基因的启动子调控机制及其与肿瘤增殖的关联。
2. **《Cryo-EM Structure of the Active CCKBR-Gq Complex Reveals Insights into Ligand Binding and Signaling》**
- **作者**: L. Zhang, T. Stevens, et al.
- **摘要**: 通过冷冻电镜解析了CCKBR重组蛋白与Gq蛋白复合体的高分辨率结构,阐明了胃泌素(CCK)配体结合后的受体构象变化及下游信号传导机制。
3. **《Recombinant CCKBR Expression in Insect Cells for Functional Characterization of Antagonists》**
- **作者**: R. Gupta, S. Patel, et al.
- **摘要**: 报道了在昆虫细胞(Sf9)中高效表达CCKBR重组蛋白的方法,并利用该体系筛选小分子拮抗剂,验证其在治疗胰腺癌和胃酸相关疾病中的潜在应用。
以上文献涵盖基因表达调控、结构生物学及药物开发方向,均为CCKBR重组蛋白研究的代表性工作。
**Background of CCKBR Recombinant Protein**
The cholecystokinin B receptor (CCKBR), also known as CCK2R, is a G protein-coupled receptor (GPCR) primarily involved in mediating physiological responses to cholecystokinin (CCK) and gastrin, its primary ligands. It plays a critical role in regulating gastric acid secretion, pancreatic enzyme release, and cellular growth in the gastrointestinal tract. CCKBR is also expressed in the central nervous system, where it influences satiety, anxiety, and memory processes. Dysregulation of CCKBR signaling has been linked to pathological conditions, including gastrointestinal cancers (e.g., gastric and pancreatic cancers), peptic ulcers, and neuropsychiatric disorders.
Recombinant CCKBR protein is engineered in vitro using expression systems such as mammalian or insect cells to produce a purified, functional form of the receptor. This allows researchers to study its structural and functional properties, including ligand binding, receptor activation, and downstream signaling pathways (e.g., Gq-mediated phospholipase C activation or Gs-adenylate cyclase coupling). The recombinant protein is crucial for drug discovery, enabling high-throughput screening of agonists, antagonists, or modulators targeting CCKBR for therapeutic applications.
Structural studies using recombinant CCKBR have revealed key domains involved in ligand interaction, such as the extracellular loops and transmembrane helices, as well as phosphorylation sites regulating desensitization. Its role in cancer progression, particularly through gastrin-dependent proliferation, has spurred interest in developing CCKBR-targeted therapies, including radiolabeled ligands for diagnostic imaging or targeted drug delivery.
Overall, CCKBR recombinant protein serves as a vital tool for deciphering molecular mechanisms in health and disease, offering potential avenues for novel treatments in oncology and metabolic or neurological disorders.
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