纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CYP3A5 |
Uniprot No | P20815 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-502aa |
氨基酸序列 | MDLIPNLAVETWLLLAVSLVLLYLYGTRTHGLFKRLGIPGPTPLPLLGNVLSYRQGLWKFDTECYKKYGKMWGTYEGQLPVLAITDPDVIRTVLVKECYSVFTNRRSLGPVGFMKSAISLAEDEEWKRIRSLLSPTFTSGKLKEMFPIIAQYGDVLVRNLRREAEKGKPVTLKDIFGAYSMDVITGTSFGVNIDSLNNPQDPFVESTKKFLKFGFLDPLFLSIILFPFLTPVFEALNVSLFPKDTINFLSKSVNRMKKSRLNDKQKHRLDFLQLMIDSQNSKETESHKALSDLELAAQSIIFIFAGYETTSSVLSFTLYELATHPDVQQKLQKEIDAVLPNKAPPTYDAVVQMEYLDMVVNETLRLFPVAIRLERTCKKDVEINGVFIPKGSMVVIPTYALHHDPKYWTEPEEFRPERFSKKKDSIDPYIYTPFGTGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLDTQGLLQPEKPIVLKVDSRDGTLSGE |
预测分子量 | 61.2 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3篇关于CYP3A5重组蛋白的参考文献及摘要概括:
1. **"Functional characterization of 25 CYP3A5 variants and assessment of enzymatic activity using diclofenac as a substrate"**
- **作者**: S. K. Kim et al.
- **摘要**: 本研究利用杆状病毒-昆虫细胞系统表达25种CYP3A5遗传变异体,评估其对双氯芬酸代谢活性的影响。结果表明,部分变异体(如CYP3A5*3)的酶活性显著降低,揭示了基因多态性对药物代谢个体差异的潜在机制。
2. **"Comparative analysis of CYP3A5 expression in Escherichia coli and human liver cells: Implications for drug metabolism studies"**
- **作者**: H. Yamazaki et al.
- **摘要**: 通过在大肠杆菌和哺乳动物细胞中重组表达CYP3A5.对比其催化活性及稳定性。发现哺乳动物系统表达的蛋白更接近天然构象,对咪达唑仑的氧化代谢活性更高,为体外药物代谢模型选择提供依据。
3. **"Role of CYP3A5 in the metabolism of HIV protease inhibitors: Insights from recombinant enzyme assays"**
- **作者**: C. A. Lee et al.
- **摘要**: 利用重组CYP3A5蛋白研究其对洛匹那韦等HIV蛋白酶抑制剂的代谢作用。实验证实CYP3A5与CYP3A4存在底物重叠性,但催化效率较低,提示两者在抗病毒药物清除中的协同作用及临床剂量调整需求。
注:以上文献信息为示例性概括,实际文献需通过PubMed/Google Scholar检索确认。
CYP3A5 is a member of the cytochrome P450 superfamily, a group of enzymes critical for metabolizing xenobiotics, drugs, and endogenous compounds. Primarily expressed in the liver, intestine, and kidney, CYP3A5 plays a significant role in the oxidative metabolism of approximately 50% of clinically used drugs, including immunosuppressants, antidepressants, and chemotherapeutic agents. Unlike its closely related isoform CYP3A4. CYP3A5 exhibits substantial genetic polymorphism, with variable expression across populations. A key single-nucleotide polymorphism (SNP), CYP3A5*3 (rs776746), results in a splicing defect that leads to non-functional protein in approximately 80–90% of Caucasians and Asians, making CYP3A5 expression highly dependent on individual genotype.
Recombinant CYP3A5 protein is engineered to study the enzyme's structure, function, and interaction with substrates or inhibitors in vitro. Produced using heterologous expression systems such as Escherichia coli, yeast, or insect cells (e.g., baculovirus-driven Sf9 cells), the recombinant protein retains catalytic activity when reconstituted with cytochrome P450 reductase and lipid cofactors. This allows researchers to dissect its metabolic contributions independently of other CYP3A isoforms, particularly CYP3A4. which often complicates in vivo studies due to overlapping substrate specificity.
CYP3A5 recombinant protein is pivotal in drug development for predicting pharmacokinetics, drug-drug interactions, and interindividual variability in drug response. Its polymorphic nature underscores its relevance in personalized medicine, as CYP3A5 expressers ("*1 allele carriers") may require dose adjustments for certain drugs. Additionally, the protein aids in mechanistic studies of enzyme induction, inhibition, and genetic variability impacts on drug metabolism. Despite structural similarities to CYP3A4. differences in substrate affinity and catalytic efficiency highlight the need for isoform-specific research, driving the demand for high-quality recombinant CYP3A5 in pharmacological and toxicological investigations.
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