| 纯度 | >85%SDS-PAGE. |
| 种属 | Human |
| 靶点 | ROS1 |
| Uniprot No | P08922 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 1881-2347aa |
| 氨基酸序列 | VWHRRLKNQKSAKEGVTVLINEDKELAELRGLAAGVGLANACYAIHTLPT QEEIENLPAFPREKLTLRLLLGSGAFGEVYEGTAVDILGVGSGEIKVAVK TLKKGSTDQEKIEFLKEAHLMSKFNHPNILKQLGVCLLNEPQYIILELME GRDLLTYLRKARMATFYGPLLTLVDLVDLCVDISKGCVYLERMHFIHRDL AARNCLVSVKDYTSPRIVKIGDFGLARDIYKNDYYRKRGEGLLPVRWMAP ESLMDGIFTTQSDVWSFGILIWEILTLGHQPYPAHSNLDVLNYVQTGGRL EPPRNCPDDLWNLMTQCWAQEPDQRPTFHRIQDQLQLFRNFFLNSIYKSR DEANNSGVINESFEGEDGDVICLNSDDIMPVALMETKNREGLNYMVLATE CGQGEEKSEGPLGSQESESCGLRKEEKEPHADKDFCQEKQVAYCPSGKPE GLNYACLTHSGYGDGSD |
| 预测分子量 | 82 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. |
1. **"Structural characterization of the ROS1 receptor tyrosine kinase and its oncogenic activation"**
- **作者**: Davare MA, et al.
- **摘要**: 本研究通过X射线晶体学解析了ROS1激酶结构域的三维结构，揭示了其致癌融合蛋白(如CD74-ROS1)中激酶活性的异常激活机制，为靶向抑制剂设计提供了结构基础。
2. **"ROS1 fusion proteins in cancer: Signaling mechanisms and therapeutic targeting"**
- **作者**: Christensen JG, et al.
- **摘要**: 文章系统总结了ROS1融合蛋白(如SLC34A2-ROS1)在肺癌等癌症中的致癌作用，通过激活下游MAPK和PI3K通路促进肿瘤生长，并探讨了小分子抑制剂(如克唑替尼)的临床前研究进展。
3. **"In vitro and in vivo activity of crizotinib in ROS1-rearranged cancers"**
- **作者**: Drilon A, et al.
- **摘要**: 该研究通过体外细胞实验和小鼠模型验证了克唑替尼对ROS1重组蛋白阳性肿瘤的选择性抑制作用，并报告了早期临床试验中患者的显著缓解率，推动了ROS1靶向治疗的临床转化。
4. **"Resistance mechanisms to ROS1-targeted therapy in non-small cell lung cancer"**
- **作者**: Zou HY, et al.
- **摘要**: 分析了ROS1抑制剂治疗后耐药性的分子机制，发现ROS1激酶域的二次突变(如G2032R)或旁路信号激活(如EGFR通路)是主要耐药原因，并提出了联合用药策略以克服耐药。
(注：上述文献标题与作者为模拟示例，实际引用需以真实文献为准。)
ROS1 (c-ros oncogene 1) is a receptor tyrosine kinase encoded by the *ROS1* gene, initially identified in 1986 through its homology with viral oncogenes. It plays a role in cellular processes like growth, differentiation, and survival. Normally, ROS1 activity is tightly regulated, but chromosomal rearrangements (e.g., fusions with CD74. SLC34A2) can lead to constitutive kinase activation, driving oncogenesis. These rearrangements are most notably associated with non-small cell lung cancer (NSCLC), occurring in 1–2% of cases, but also appear in gliomas, cholangiocarcinomas, and other malignancies.
ROS1 recombinant proteins are engineered versions of the kinase domain or fusion variants produced in vitro using expression systems like *E. coli* or mammalian cells. These proteins retain the enzymatic activity and structural features of native ROS1. making them critical tools for biochemical assays, drug screening, and mechanistic studies. For example, recombinant ROS1 kinase domains are used to test inhibitor efficacy, map drug-binding sites, or study resistance mutations (e.g., G2032R) that arise in response to targeted therapies like crizotinib.
The development of ROS1-targeted therapies relies heavily on recombinant protein-based research. First-generation inhibitors (crizotinib, entrectinib) and next-generation drugs (lorlatinib, repotrectinib) were validated using kinase assays and structural studies involving recombinant ROS1. Additionally, recombinant proteins aid in diagnostic applications, such as antibody validation for immunohistochemistry to detect ROS1 fusions in patient samples.
Despite progress, challenges persist, including understanding heterogeneous fusion partners and optimizing therapies to penetrate the blood-brain barrier. Recombinant ROS1 proteins continue to support efforts to unravel signaling pathways, model resistance mechanisms, and design novel inhibitors, underscoring their importance in translational oncology.
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