纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CYP2D6 |
Uniprot No | P10635 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 236-472aa |
氨基酸序列 | LAGKV LRFQKAFLTQ LDELLTEHRM TWDPAQPPRD LTEAFLAEME KAKGNPESSF NDENLRIVVA DLFSAGMVTT STTLAWGLLL MILHPDVQRR VQQEIDDVIG QVRRPEMGDQ AHMPYTTAVI HEVQRFGDIV PLGVTHMTSR DIEVQGFRIP KGTTLITNLS SVLKDEAVWE KPFRFHPEHF LDAQGHFVKP EAFLPFSAGR RACLGEPLAR MELFLFFTSL LQHFSFSVPT GQ |
预测分子量 | 56 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CYP2D6重组蛋白的3篇文献示例(注:以下为模拟参考文献,实际引用请核实原文):
1. **"Heterologous expression of human CYP2D6 in Escherichia coli: Optimization and catalytic activity analysis"**
- **作者**: Smith J, et al.
- **摘要**: 研究通过在大肠杆菌中表达CYP2D6重组蛋白,优化了诱导条件和载体设计,成功获得高活性酶,并证明其代谢右美沙芬的能力与哺乳动物系统相当。
2. **"Functional characterization of recombinant CYP2D6 variants using a baculovirus-insect cell system"**
- **作者**: Wang L, et al.
- **摘要**: 利用杆状病毒-昆虫细胞系统表达多种CYP2D6基因多态性变体,通过质谱分析揭示了不同突变体对β-受体阻滞剂代谢的动力学差异。
3. **"Reconstitution of CYP2D6-mediated drug metabolism in vitro using purified recombinant enzyme and NADPH-cytochrome P450 reductase"**
- **作者**: Gonzalez FJ, et al.
- **摘要**: 通过共表达CYP2D6和NADPH-P450还原酶,建立体外药物代谢模型,验证了其对曲马多和阿米替林的氧化代谢活性,为药物相互作用研究提供工具。
4. **"Improving the solubility and stability of recombinant CYP2D6 for high-throughput screening assays"**
- **作者**: Patel R, et al.
- **摘要**: 通过添加亲水标签和突变疏水残基,提高CYP2D6重组蛋白的可溶性和稳定性,成功应用于药物候选化合物的高通量代谢稳定性测试。
(注:以上文献信息为示例,实际文献需通过学术数据库检索确认。)
CYP2D6 is a member of the cytochrome P450 enzyme superfamily, primarily expressed in the liver, and plays a critical role in the metabolism of approximately 25% of clinically used drugs, including antidepressants, antipsychotics, beta-blockers, and opioids. It is highly polymorphic, with over 100 known genetic variants, leading to significant interindividual differences in enzyme activity categorized as poor, intermediate, extensive, or ultrarapid metabolizers. These genetic variations profoundly influence drug efficacy, toxicity, and personalized dosing strategies.
Recombinant CYP2D6 protein is engineered using heterologous expression systems (e.g., bacteria, yeast, or mammalian cells) to produce functional enzyme for *in vitro* studies. This technology allows large-scale production of the protein, enabling researchers to investigate substrate specificity, enzyme kinetics, and drug-drug interactions without confounding factors present in human tissue samples. Recombinant CYP2D6 is widely used in pharmaceutical research to predict metabolic stability, identify potential metabolites, and assess the impact of genetic polymorphisms on drug metabolism.
Additionally, it serves as a tool for structural studies, such as X-ray crystallography and molecular modeling, to elucidate mechanisms of substrate binding and catalysis. The development of recombinant CYP2D6 has advanced pharmacogenomics by facilitating high-throughput screening of polymorphic variants and improving *in vitro-in vivo* extrapolation (IVIVE) for drug development. However, challenges remain in replicating the native enzyme's membrane-bound environment and interactions with cytochrome P450 reductase, which can affect activity measurements. Despite these limitations, recombinant CYP2D6 remains indispensable for mechanistic studies and optimizing therapeutic regimens tailored to individual genetic profiles.
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