| 纯度 | >85%SDS-PAGE. |
| 种属 | Human |
| 靶点 | DOT1L |
| Uniprot No | Q8TEK3 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 1-435aa |
| 氨基酸序列 | MGEKLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPD LKLAMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTTQPMKLNT RPSTGLLRHILQQVYNHSVTDPEKLNNYEPFSPEVYGETSFDLVAQMIDE IKMTDDDLFVDLGSGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDR EFRKWMKWYGKKHAEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVD HQLKERFANMKEGGRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLK GSVSWTGKPVSYYLHTIDRTILENYFSSLKNPKLREEQEAARRRQQRESK SNAATPTKGPEGKVAGPADAPMDSGAEEEKAGAATVKKPSPSKARKKKLN KKGRKMAGRKRGRPKKMNTANPERKPKKNQTALDA |
| 预测分子量 | 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DOT1L重组蛋白的3篇代表性文献及其摘要内容：
---
1. **"Structural basis for DOT1L-mediated methylation of H3K79 and its inhibition by engineered proteins"**
*作者：Valencia-Sánchez, M.I. et al. (2019)*
**摘要**：本研究通过重组表达人源DOT1L蛋白，结合X射线晶体学解析了DOT1L与核小体复合物的结构，揭示了其特异性甲基化组蛋白H3K79的分子机制，并设计了工程化蛋白抑制剂阻断其活性。
2. **"DOT1L methylates H3K79 and promotes oncogenic transcription in leukemia"**
*作者：Nguyen, A.T. et al. (2011)*
**摘要**：通过体外重组DOT1L蛋白的活性实验，证明其与MLL融合蛋白的相互作用可驱动H3K79高甲基化，进而激活白血病相关基因的异常转录，为靶向DOT1L的癌症治疗提供依据。
3. **"Development of a high-throughput screening assay for DOT1L histone methyltransferase inhibitors using recombinant protein"**
*作者：Zhang, W. et al. (2016)*
**摘要**：研究报道了一种基于重组人DOT1L蛋白的高通量筛选平台，用于鉴定新型小分子抑制剂，并验证了其选择性抑制H3K79甲基化的活性，为药物开发奠定基础。
---
这些文献涵盖了DOT1L重组蛋白的结构解析、功能机制及抑制剂开发方向，均涉及重组蛋白的体外表达与活性分析。如需具体期刊或补充信息，可进一步检索PubMed或相关数据库。
**Background of DOT1L Recombinant Protein**
DOT1L (Disruptor of Telomeric Silencing 1-Like) is a conserved histone methyltransferase that catalyzes the methylation of histone H3 on lysine 79 (H3K79), a post-translational modification linked to transcriptional regulation, DNA repair, and cell cycle progression. Unlike most histone methyltransferases that target lysine residues on histone tails, DOT1L specifically methylates H3K79 located within the globular core of nucleosomes. This unique activity requires its interaction with ubiquitinated histone H2B, highlighting its role in cross-talk between histone modifications.
Recombinant DOT1L protein is engineered for *in vitro* studies to dissect its enzymatic mechanisms, structural features, and interactions. Produced in heterologous systems (e.g., *E. coli* or insect cells), the recombinant protein often includes affinity tags (e.g., GST or His-tags) to facilitate purification. Its applications span biochemical assays (e.g., methylation kinetics), inhibitor screening (for therapeutic development), and structural studies (e.g., X-ray crystallography or cryo-EM) to map catalytic domains or binding interfaces.
DOT1L gained prominence due to its involvement in MLL (mixed-lineage leukemia)-rearranged leukemias, where aberrant H3K79 methylation drives oncogenic gene expression. Inhibitors like EPZ-5676 (pinometostat), developed using recombinant DOT1L in preclinical studies, have entered clinical trials, underscoring its therapeutic relevance. Beyond cancer, DOT1L dysregulation is implicated in developmental disorders and cardiac hypertrophy.
The availability of recombinant DOT1L protein accelerates mechanistic studies and drug discovery, offering a tool to explore epigenetic regulation and validate targeted therapies. Its study continues to reveal insights into chromatin dynamics and disease pathogenesis, positioning DOT1L as a critical target in precision medicine.
×
