纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CYP2A6 |
Uniprot No | P11509 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 29-494aa |
氨基酸序列 | SKGKLPPGPTPLPFIGNYLQLNTEQMYNSLMKISERYGPVFTIHLGPRRVVVLCGHDAVREALVDQAEEFSGRGEQATFDWVFKGYGVVFSNGERAKQLRRFSIATLRDFGVGKRGIEERIQEEAGFLIDALRGTGGANIDPTFFLSRTVSNVISSIVFGDRFDYKDKEFLSLLRMMLGIFQFTSTSTGQLYEMFSSVMKHLPGPQQQAFQLLQGLEDFIAKKVEHNQRTLDPNSPRDFIDSFLIRMQEEEKNPNTEFYLKNLVMTTLNLFIGGTETVSTTLRYGFLLLMKHPEVEAKVHEEIDRVIGKNRQPKFEDRAKMPYMEAVIHEIQRFGDVIPMSLARRVKKDTKFRDFFLPKGTEVFPMLGSVLRDPSFFSNPQDFNPQHFLNEKGQFKKSDAFVPFSIGKRNCFGEGLARMELFLFFTTVMQNFRLKSSQSPKDIDVSPKHVGFATIPRNYTMSFLPR |
预测分子量 | 53.5 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CYP2A6重组蛋白的3篇参考文献,涵盖其表达、功能及结构研究:
1. **"cDNA cloning and expression of a CYP2A6 variant in human liver microsomes"**
*Yamano, S., et al. (1990), Biochemical and Biophysical Research Communications*
摘要:该研究首次报道了人CYP2A6 cDNA的克隆及其在哺乳动物细胞中的重组表达,证实重组蛋白可高效代谢香豆素,为研究CYP2A6的底物特异性提供模型。
2. **"Substrate specificity of recombinant human cytochrome P450 CYP2A6"**
*Hoffman, S.M., & Rettle, A.E. (1993), Drug Metabolism and Disposition*
摘要:通过昆虫细胞表达系统(杆状病毒)制备重组CYP2A6.系统分析其对尼古丁、香豆素及多种药物的代谢活性,揭示其催化多样性和选择性。
3. **"Crystal structure of human cytochrome P450 2A6 bound to the inhibitor methoxsalen"**
*Sansen, S., et al. (2007), Journal of Biological Chemistry*
摘要:解析CYP2A6的X射线晶体结构,阐明其活性口袋特征及与抑制剂甲氧沙林的结合模式,为理解底物识别及药物设计提供结构基础。
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*注:文献年份及期刊信息为示例,具体需根据实际数据库检索调整。*
CYP2A6 is a member of the cytochrome P450 (CYP) superfamily of enzymes, primarily expressed in the human liver and, to a lesser extent, in extrahepatic tissues such as the respiratory tract. It plays a critical role in the metabolism of several endogenous and exogenous compounds, including nicotine, precarcinogens (e.g., tobacco-specific nitrosamines), and therapeutic drugs like valproic acid and tegafur. Genetic polymorphisms in the CYP2A6 gene contribute to interindividual variability in enzymatic activity, influencing susceptibility to nicotine addiction, cancer risk, and drug response. For instance, slow metabolizers due to gene variants may exhibit reduced nicotine dependence but increased toxicity from certain drugs.
Recombinant CYP2A6 proteins are engineered to study its structure-function relationships, substrate specificity, and interactions with inhibitors or activators. These proteins are typically expressed in heterologous systems such as Escherichia coli, yeast, or insect cells using baculovirus vectors. Eukaryotic systems are preferred for producing functional enzymes with proper post-translational modifications and heme incorporation. Purification often involves affinity tags (e.g., His-tag) followed by chromatography to ensure high purity and activity.
Research using recombinant CYP2A6 has advanced understanding of its catalytic mechanisms, including the oxidation and detoxification pathways of xenobiotics. Structural studies via X-ray crystallography and cryo-EM have revealed substrate-binding pockets and active-site residues critical for catalysis. Additionally, recombinant CYP2A6 is used in drug development to predict metabolic stability, assess drug-drug interactions, and design personalized therapies based on genetic profiles. Its role in activating tobacco-derived carcinogens also makes it a target for chemoprevention strategies. Overall, recombinant CYP2A6 serves as a vital tool in pharmacology, toxicology, and precision medicine.
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