纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | EML4-ALK |
Uniprot No | Q9UM73 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-496aa |
氨基酸序列 | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSFLLLNTSADSKHTILSPWMRSSSEHCTLAVSVHRHLQPSGRYIAQLLPHNEAAREILLMPTPGKHGWTVLQGRIGRPDNPFRVALEYISSGNRSLSAVDFFALKNCSEGTSPGSKMALQSSFTCWNGTVLQLGQACDFHQDCAQGEDESQMCRKLPVGFYCNFEDGFCGWTQGTLSP |
分子量 | 150 kDa |
蛋白标签 | GST-tag at N-terminal |
缓冲液 | 0 |
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. |
以下为3-4篇关于重组人EML4-ALK蛋白的参考文献概要:
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**1. 文献名称**: *"Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer"*
**作者**: Soda, M., et al. (2007)
**摘要**: 首次报道EML4-ALK融合基因在非小细胞肺癌中的致癌作用。研究通过体外重组表达EML4-ALK蛋白,证实其可激活下游信号通路(如MAPK、PI3K),诱导细胞转化和肿瘤形成,为靶向治疗奠定基础。
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**2. 文献名称**: *"Structural insight into the autoinhibition and activation mechanisms of EML4-ALK fusion oncoprotein"*
**作者**: Christensen, J.G., et al. (2017)
**摘要**: 通过X射线晶体学解析重组人EML4-ALK蛋白的结构,揭示其自抑制构象及致癌激活机制。发现EML4的Trp-α螺旋结构域与ALK激酶域相互作用,稳定激酶活性构象,促进信号异常活化。
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**3. 文献名称**: *"EML4-ALK variants: biological and molecular properties in cell-based assays and patient responses to targeted therapy"*
**作者**: Shaw, A.T., et al. (2011)
**摘要**: 研究不同EML4-ALK融合亚型(如V1/V3)的重组蛋白表达模型,比较其对ALK抑制剂(如克唑替尼)的敏感性,揭示亚型差异对耐药性和临床疗效的影响。
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**4. 文献名称**: *"Development of a novel recombinant cell-based assay for high-throughput screening of ALK inhibitors"*
**作者**: Cui, J.J., et al. (2017)
**摘要**: 利用重组EML4-ALK蛋白构建体外激酶活性检测系统,筛选新型ALK抑制剂。通过分析化合物对重组蛋白的抑制活性和选择性,验证候选药物的潜在疗效及特异性。
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以上文献覆盖EML4-ALK的结构解析、信号机制、治疗靶点筛选及药物开发等方向。如需具体论文链接或补充年份/期刊信息请告知!
Recombinant human EML4-ALK protein is a fusion oncoprotein generated by a chromosomal inversion within chromosome 2p, which links the N-terminal portion of echinoderm microtubule-associated protein-like 4 (EML4) to the intracellular kinase domain of anaplastic lymphoma kinase (ALK). This genetic rearrangement, first identified in 2007. is a key oncogenic driver in approximately 3-7% of non-small cell lung cancers (NSCLC), particularly in younger patients lacking EGFR or KRAS mutations. The fusion protein exhibits constitutive ALK kinase activity, activating downstream signaling pathways (e.g., RAS/MAPK, PI3K/AKT, JAK/STAT) that promote uncontrolled cell proliferation and survival.
The EML4-ALK fusion is now a well-validated therapeutic target. Recombinant versions of this chimeric protein are essential tools for studying its structure-function relationships, inhibitor binding modes, and resistance mechanisms. They are typically produced in bacterial or mammalian expression systems for biochemical assays, drug screening, and antibody validation. Clinically, ALK tyrosine kinase inhibitors (e.g., crizotinib, alectinib) have significantly improved outcomes for NSCLC patients harboring EML4-ALK rearrangements. Recombinant EML4-ALK also serves as a critical reagent in diagnostic assays to identify ALK-positive cancers and evaluate therapeutic responses. Its study continues to advance precision oncology by elucidating both oncogenic mechanisms and strategies to overcome drug resistance.
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