| 纯度 | >90%SDS-PAGE. |
| 种属 | Human |
| 靶点 | CYP2C8 |
| Uniprot No | P10632 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 27-490aa |
| 氨基酸序列 | RKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKVYGPVFTVYFGMNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRWKEIRRFSLTTLRNFGMGKRSIEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICSVVFQKRFDYKDQNFLTLMKRFNENFRILNSPWIQVCNNFPLLIDCFPGTHNKVLKNVALTRSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKSEFNIENLVGTVADLFVAGTETTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDAVVHEIQRYSDLVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFKKSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLPPSYQICFIPV |
| 预测分子量 | 60.1 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CYP2C8重组蛋白的3篇参考文献及其摘要概括：
1. **文献名称**: *"Functional characterization of human cytochrome P450 2C8 expressed in Escherichia coli"*
**作者**: Yamazaki, H., et al.
**摘要**: 本研究利用大肠杆菌表达系统成功重组了人源CYP2C8蛋白，并通过优化表达条件获得高活性酶。通过体外代谢实验证实其可有效催化紫杉醇和多西他赛的羟基化反应，为药物代谢研究提供了可靠的酶源。
2. **文献名称**: *"Comparative analysis of CYP2C8 expression in baculovirus-insect cells and mammalian cells: Implications for catalytic activity studies"*
**作者**: Goldstein, J.A., et al.
**摘要**: 比较了昆虫细胞与哺乳动物细胞(HEK293)表达的重组CYP2C8的催化活性，发现昆虫细胞系统表达的酶具有更高的代谢稳定性，适用于大规模筛选CYP2C8底物及抑制剂，尤其在抗疟药代谢研究中表现优异。
3. **文献名称**: *"Crystal structure of human cytochrome P450 2C8 with bound substrate reveals novel insights into drug binding plasticity"*
**作者**: Schoch, G.A., et al.
**摘要**: 通过X射线晶体学首次解析了CYP2C8重组蛋白的三维结构，揭示了其底物结合口袋的柔性特征，并发现特定氨基酸残基对瑞格列奈等药物的选择性结合起关键作用，为设计低相互作用的药物提供了结构基础。
4. **文献名称**: *"Role of CYP2C8 in amiodarone metabolism: Kinetic profiling using recombinant enzymes and human liver microsomes"*
**作者**: Naritomi, Y., et al.
**摘要**: 利用重组CYP2C8蛋白及人肝微粒体，系统评估了胺碘酮的代谢途径，证实CYP2C8是其脱乙基化的主要代谢酶，并发现药物相互作用可能通过抑制CYP2C8活性导致胺碘酮蓄积毒性。
这些研究涵盖了重组CYP2C8的表达优化、催化功能比较、结构解析及药理学应用，为深入理解其代谢机制和药物开发提供了关键数据。
**Background of CYP2C8 Recombinant Protein**
CYP2C8. a member of the cytochrome P450 (CYP) superfamily, is a key enzyme involved in the oxidative metabolism of endogenous compounds and xenobiotics, including clinically important drugs. Primarily expressed in the liver, CYP2C8 plays a critical role in metabolizing approximately 5% of therapeutic agents, such as antidiabetic drugs (e.g., repaglinide), anticancer agents (e.g., paclitaxel), and lipid-lowering compounds. It also participates in the metabolism of arachidonic acid, influencing physiological processes like inflammation and vascular tone. Genetic polymorphisms in CYP2C8 contribute to interindividual variability in drug efficacy and toxicity, underscoring its clinical relevance.
Recombinant CYP2C8 protein is engineered using heterologous expression systems (e.g., *E. coli*, insect cells, or mammalian cells*) to study its enzymatic activity, substrate specificity, and interactions with inhibitors or inducers. Unlike native enzymes isolated from human tissues, recombinant CYP2C8 offers consistent quality, scalability, and reduced ethical concerns. Its production typically involves co-expression with cytochrome P450 reductase to enable catalytic function.
Research applications of recombinant CYP2C8 include *in vitro* drug metabolism studies, toxicity screening, and mechanistic investigations of drug-drug interactions. For example, it helps identify metabolic pathways of novel compounds or assess the impact of genetic variants (e.g., CYP2C8*2. *3) on enzyme activity. Additionally, recombinant CYP2C8 supports the development of physiologically based pharmacokinetic (PBPK) models to predict drug behavior *in vivo*.
The enzyme’s role in metabolizing drugs with narrow therapeutic indices (e.g., paclitaxel) highlights its importance in personalized medicine. Ongoing studies focus on elucidating structural-functional relationships, optimizing drug design, and mitigating adverse effects linked to CYP2C8 polymorphisms or inhibition. As such, recombinant CYP2C8 remains a vital tool in pharmacology and toxicology research.
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