纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | EZH2 |
Uniprot No | Q15910 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-746aa |
氨基酸序列 | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP |
预测分子量 | 86.8 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EZH2重组蛋白的3篇代表性文献的简要信息:
1. **文献名称**:*Structural basis of EZH2 recognition by small-molecule inhibitors*
**作者**:Vermeulen, M. et al.
**摘要**:该研究通过X射线晶体学解析了EZH2重组蛋白的催化结构域与抑制剂复合物的三维结构,揭示了抑制剂结合的关键位点,为靶向EZH2的抗癌药物设计提供了结构基础。
2. **文献名称**:*EZH2 oncogenic mutations drive epigenetic, transcriptional, and structural changes in chromatin*
**作者**:Jiao, L. et al.
**摘要**:文章利用重组EZH2蛋白(野生型和突变型)进行体外甲基转移酶活性分析,发现致癌突变体(如Y641N)显著增强H3K27me3催化效率,并改变染色质结构,促进癌症发生。
3. **文献名称**:*A cell-free assay for the enzymatic activity of EZH2 and its inhibition by small molecules*
**作者**:McCabe, M.T. et al.
**摘要**:作者建立了基于重组EZH2蛋白的体外酶活性检测体系,筛选并验证了多种小分子抑制剂(如GSK126)对EZH2甲基转移酶活性的特异性抑制作用,为药物开发提供工具。
4. **文献名称**:*Recombinant EZH2 expression and purification for biochemical characterization*
**作者**:Wu, Z. et al.
**摘要**:该文献详细描述了人源EZH2重组蛋白在大肠杆菌中的表达和纯化方法,优化了其酶活条件,并验证了其与SUZ12、EED等PRC2复合体亚基的功能互作。
以上研究覆盖了EZH2重组蛋白的结构解析、突变功能分析、抑制剂筛选及实验方法开发等方向。
EZH2 (Enhancer of Zeste Homolog 2) is a catalytic subunit of the Polycomb Repressive Complex 2 (PRC2), a critical epigenetic regulator involved in gene silencing through histone modification. It mediates the trimethylation of histone H3 on lysine 27 (H3K27me3), a repressive chromatin mark that promotes transcriptional repression by compacting chromatin structure. EZH2 plays essential roles in cell differentiation, cell cycle regulation, and maintaining stem cell pluripotency. Dysregulation of EZH2 is strongly associated with various cancers, including lymphomas, breast cancer, and prostate cancer, where its overexpression or gain-of-function mutations drive uncontrolled cell proliferation and metastasis.
Recombinant EZH2 proteins are engineered in vitro using expression systems like *E. coli* or mammalian cells to produce highly purified, functional forms of the enzyme for research and therapeutic development. These proteins retain the SET domain responsible for methyltransferase activity, enabling studies on PRC2 complex assembly, substrate specificity, and inhibition mechanisms. Recombinant EZH2 is widely used in biochemical assays (e.g., enzyme activity profiling, inhibitor screening), structural studies (crystallography, cryo-EM), and cell-based models to explore its pathological roles.
Pharmaceutical interest in EZH2 has surged due to its potential as a therapeutic target. Small-molecule inhibitors (e.g., tazemetostat, GSK126) designed using recombinant EZH2 models show promise in clinical trials for treating EZH2-driven malignancies. Additionally, recombinant proteins facilitate biomarker discovery and personalized medicine strategies by correlating EZH2 activity with disease progression. Challenges remain in understanding context-dependent functions and off-target effects, underscoring the need for high-quality recombinant tools to dissect EZH2's complex biology and advance targeted therapies.
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