纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | KEAP1 |
Uniprot No | Q14145 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-624aa |
氨基酸序列 | MQPDPRPSGAGACCRFLPLQSQCPEGAGDAVMYASTECKAEVTPSQHGNR TFSYTLEDHTKQAFGIMNELRLSQQLCDVTLQVKYQDAPAAQFMAHKVVL ASSSPVFKAMFTNGLREQGMEVVSIEGIHPKVMERLIEFAYTASISMGEK CVLHVMNGAVMYQIDSVVRACSDFLVQQLDPSNAIGIANFAEQIGCVELH QRAREYIYMHFGEVAKQEEFFNLSHCQLVTLISRDDLNVRCESEVFHACI NWVKYDCEQRRFYVQALLRAVRCHSLTPNFLQMQLQKCEILQSDSRCKDY LVKIFEELTLHKPTQVMPCRAPKVGRLIYTAGGYFRQSLSYLEAYNPSDG TWLRLADLQVPRSGLAGCVVGGLLYAVGGRNNSPDGNTDSSALDCYNPMT NQWSPCAPMSVPRNRIGVGVIDGHIYAVGGSHGCIHHNSVERYEPERDEW HLVAPMLTRRIGVGVAVLNRLLYAVGGFDGTNRLNSAECYYPERNEWRMI TAMNTIRSGAGVCVLHNCIYAAGGYDGQDQLNSVERYDVETETWTFVAPM KHRRSALGITVHQGRIYVLGGYDGHTFLDSVECYDPDTDTWSEVTRMTSG RSGVGVAVTMEPCRKQIDQQNCTC |
预测分子量 | 71 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KEAP1重组蛋白的3篇代表性文献(部分信息为示例性虚构,实际引用时请核实原文):
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1. **文献名称**:*Structural and functional analysis of recombinant KEAP1 protein in Nrf2 regulation*
**作者**:Suzuki, T., et al.
**摘要**:本研究通过重组表达纯化KEAP1蛋白,验证其与Nrf2的结合能力,并证明氧化应激条件下KEAP1构象变化导致Nrf2释放,激活抗氧化反应元件(ARE)通路。
2. **文献名称**:*Development of a high-throughput screening platform using recombinant KEAP1 for Nrf2 inhibitors*
**作者**:Zhang, D.D., et al.
**摘要**:利用重组KEAP1蛋白建立体外药物筛选模型,成功鉴定出小分子化合物通过竞争性结合KEAP1 Kelch结构域激活Nrf2.为抗氧化治疗提供候选药物。
3. **文献名称**:*Crystal structure of KEAP1-DC domain complex reveals mechanistic insights into ubiquitination*
**作者**:Yamamoto, M., et al.
**摘要**:解析重组KEAP1双甘氨酸结构域(DC)的晶体结构,阐明其介导Nrf2泛素化降解的分子机制,为靶向KEAP1-Nrf2相互作用的药物设计提供结构基础。
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如需实际文献,建议通过PubMed或Google Scholar检索关键词“recombinant KEAP1 protein”“KEAP1-Nrf2 interaction”获取。
**Background of KEAP1 Recombinant Protein**
KEAP1 (Kelch-like ECH-associated protein 1) is a critical regulatory protein involved in cellular defense mechanisms against oxidative and electrophilic stress. It functions as a substrate adaptor for the Cullin3 (CUL3)-based E3 ubiquitin ligase complex, primarily targeting the transcription factor NRF2 (Nuclear factor erythroid 2-related factor 2) for proteasomal degradation under normal conditions. Under stress, KEAP1 senses reactive oxygen species (ROS) or electrophiles through its cysteine-rich domains, leading to conformational changes that disrupt its interaction with NRF2. This allows NRF2 to accumulate, translocate to the nucleus, and activate antioxidant response element (ARE)-driven genes, which encode detoxifying enzymes and cytoprotective proteins.
The KEAP1 recombinant protein is engineered in vitro using expression systems like *E. coli* or mammalian cells, enabling researchers to study its structure-function relationships, post-translational modifications, and interactions with NRF2 or small-molecule inhibitors. Structurally, KEAP1 contains three major domains: an N-terminal Broad Complex, Tramtrack, and Bric-à-Brac (BTB) domain for dimerization and CUL3 binding, an intervening region (IVR) with stress-sensing cysteine residues, and a C-terminal Kelch repeat domain that binds NRF2.
Recombinant KEAP1 is pivotal in drug discovery, particularly for diseases linked to oxidative stress (e.g., cancer, neurodegenerative disorders) or NRF2/KEAP1 pathway dysregulation. It facilitates high-throughput screening of compounds aiming to modulate NRF2 activity—either by inhibiting KEAP1 to boost antioxidant responses or stabilizing the KEAP1-NRF2 interaction to counteract NRF2 hyperactivity in certain cancers. Additionally, studies using recombinant KEAP1 have clarified mechanisms of chemopreventive agents (e.g., sulforaphane) and informed therapeutic strategies targeting the KEAP1-NRF2 axis.
Overall, KEAP1 recombinant protein serves as a vital tool for understanding redox biology and developing therapies for stress-related pathologies.
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