纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CES2 |
Uniprot No | O00748 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 27-559aa |
氨基酸序列 | QDSASPIRTTHTGQVLGSLVHVKGANAGVQTFLGIPFAKPPLGPLRFAPPEPPESWSGVRDGTTHPAMCLQDLTAVESEFLSQFNMTFPSDSMSEDCLYLSIYTPAHSHEGSNLPVMVWIHGGALVFGMASLYDGSMLAALENVVVVIIQYRLGVLGFFSTGDKHATGNWGYLDQVAALRWVQQNIAHFGGNPDRVTIFGESAGGTSVSSLVVSPISQGLFHGAIMESGVALLPGLIASSADVISTVVANLSACDQVDSEALVGCLRGKSKEEILAINKPFKMIPGVVDGVFLPRHPQELLASADFQPVPSIVGVNNNEFGWLIPKVMRIYDTQKEMDREASQAALQKMLTLLMLPPTFGDLLREEYIGDNGDPQTLQAQFQEMMADSMFVIPALQVAHFQCSRAPVYFYEFQHQPSWLKNIRPPHMKADHGDELPFVFRSFFGGNYIKFTEEEEQLSRKMMKYWANFARNGNPNGEGLPHWPLFDQEEQYLQLNLQPAVGRALKAHRLQFWKKALPQKIQELEEPEERHTEL |
预测分子量 | 65.9 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CES2重组蛋白的3篇参考文献及其摘要概括:
1. **文献名称**:*"Expression and characterization of recombinant human carboxylesterase 2 in insect cells"*
**作者**:Hyatt, S.L., et al.
**摘要**:该研究报道了利用杆状病毒-昆虫细胞系统成功表达重组人CES2蛋白,并验证其酶活性。通过底物特异性实验发现,重组CES2对伊立替康(CPT-11)的水解活性显著,为药物代谢研究提供可靠工具。
2. **文献名称**:*"Structural basis of prodrug activation by human carboxylesterase 2"*
**作者**:Bencharit, S., et al.
**摘要**:通过X射线晶体学解析了重组CES2的三维结构,揭示了其催化口袋的关键氨基酸残基。研究阐明了CES2如何识别并水解抗肿瘤前药(如奥司他韦),为设计靶向CES2的药物提供结构基础。
3. **文献名称**:*"Functional analysis of CES2 genetic variants and their impact on drug metabolism"*
**作者**:Hosokawa, M., et al.
**摘要**:研究通过重组表达不同CES2基因变异体,评估其对多种药物(包括抗病毒和抗癌药物)的代谢能力差异。发现特定SNP(如rs11075646)显著降低酶活性,提示个体化用药的重要性。
4. **文献名称**:*"Development of a high-throughput assay for CES2 inhibition screening"*
**作者**:Wadkins, R.M., et al.
**摘要**:建立基于重组CES2蛋白的荧光底物高通量筛选平台,用于快速鉴定潜在抑制剂。研究筛选出多个小分子化合物,可能用于调节CES2介导的药物毒性或增强前药疗效。
**注**:以上文献为示例性质,实际引用时需核对原文信息及数据库(如PubMed、Web of Science)的准确性。
Carboxylesterase 2 (CES2), a key enzyme in the carboxylesterase family, plays a vital role in metabolizing ester- and amide-containing compounds, including clinical drugs, environmental toxins, and endogenous lipids. It is predominantly expressed in the liver, intestine, and kidneys, where it catalyzes hydrolysis reactions critical for drug activation, detoxification, and lipid homeostasis. Unlike its isoform CES1. CES2 exhibits distinct substrate specificity, preferentially processing bulky substrates like irinotecan (a chemotherapy prodrug) or angiotensin-converting enzyme inhibitors.
Recombinant CES2 proteins are engineered using expression systems (e.g., *E. coli*, insect, or mammalian cells*) to produce purified enzymes for functional and structural studies. These proteins enable researchers to investigate CES2's catalytic mechanisms, substrate preferences, and interactions with inhibitors or activators. Structural analyses via X-ray crystallography or cryo-EM have revealed its α/β-hydrolase fold and active-site architecture, guiding drug design for improved therapeutic efficacy.
In drug development, recombinant CES2 is used to screen prodrug activation potential or assess metabolic stability of candidate compounds. It also aids in studying interindividual variability in drug responses linked to CES2 genetic polymorphisms, which impact enzyme activity. Additionally, its role in lipid metabolism has implications for metabolic diseases, such as obesity and diabetes. Challenges in recombinant production include maintaining proper post-translational modifications (e.g., glycosylation) for optimal activity, often addressed through mammalian expression systems.
Overall, recombinant CES2 serves as a vital tool in pharmacology, toxicology, and precision medicine, bridging molecular insights to clinical applications.
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