纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CCKAR |
Uniprot No | P32238 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-428aa |
氨基酸序列 | MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNTLVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYFMGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYSNLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGIKFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNSSAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSYTSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSHMSASVPPQ |
预测分子量 | 47,8 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CCKAR重组蛋白的3篇参考文献示例,包含文献名称、作者及摘要概括:
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1. **文献名称**:*"Expression and Purification of Recombinant Human CCKAR in Baculovirus-Insect Cell System"*
**作者**:Smith J, et al.
**摘要**:研究利用杆状病毒-昆虫细胞系统高效表达人源CCKAR重组蛋白,通过亲和层析和尺寸排阻色谱纯化,获得具有配体结合活性的功能性受体,为结构研究奠定基础。
2. **文献名称**:*"Structural Insights into CCKAR Activation Using Cryo-EM"*
**作者**:Chen L, et al.
**摘要**:通过冷冻电镜解析CCKAR重组蛋白与激动剂复合物的三维结构,揭示受体激活过程中跨膜结构域的构象变化,为靶向药物设计提供依据。
3. **文献名称**:*"Functional Characterization of Recombinant CCKAR in GPCR Signaling Pathways"*
**作者**:Wang Y, et al.
**摘要**:在HEK293细胞中表达CCKAR重组蛋白,证实其通过Gq蛋白介导细胞内钙离子信号通路,并评估多种配体的效价差异,支持其在药物筛选中的应用。
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以上示例为模拟文献,实际引用时需核实具体来源及准确性。如需真实文献,建议在PubMed或Web of Science中检索关键词“CCKAR recombinant protein”。
Cholecystokinin A receptor (CCKAR), also known as CCK1R, is a G protein-coupled receptor (GPCR) primarily expressed in the gastrointestinal tract, pancreas, and central nervous system. It binds to cholecystokinin (CCK), a peptide hormone critical for regulating digestion, satiety, and anxiety. CCKAR activation triggers intracellular signaling cascades (e.g., phospholipase C pathway) that mediate gallbladder contraction, pancreatic enzyme secretion, and gut motility. Dysregulation of CCKAR signaling is implicated in metabolic disorders, obesity, and gastrointestinal pathologies, making it a therapeutic target.
Recombinant CCKAR proteins are engineered using heterologous expression systems (e.g., mammalian, insect, or bacterial cells) to produce purified receptor variants for functional studies. These proteins retain key structural features, such as seven transmembrane domains and ligand-binding specificity, enabling researchers to investigate receptor-ligand interactions, signal transduction mechanisms, and drug screening. Tagged versions (e.g., His-tag, FLAG-tag) facilitate purification, localization, or detection in assays.
The development of CCKAR recombinant proteins has advanced drug discovery, particularly for appetite modulators and gastrointestinal therapeutics. They are also used to study receptor polymorphisms, allosteric modulation, and structural dynamics via techniques like cryo-EM or X-ray crystallography. Challenges include maintaining receptor stability during purification and ensuring proper post-translational modifications (e.g., glycosylation) for native-like activity. Ongoing research aims to optimize expression platforms and engineer constitutively active mutants to broaden pharmacological applications.
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