纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | CDK8 |
Uniprot No | P49336 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-464aa |
氨基酸序列 | MDYDFKVKLS SERERVEDLF EYEGCKVGRG TYGHVYKAKR KDGKDDKDYA LKQIEGTGIS MSACREIALL RELKHPNVIS LQKVFLSHAD RKVWLLFDYA EHDLWHIIKF HRASKANKKP VQLPRGMVKS LLYQILDGIH YLHANWVLHR DLKPANILVM GEGPERGRVK IADMGFARLF NSPLKPLADL DPVVVTFWYR APELLLGARH YTKAIDIWAI GCIFAELLTS EPIFHCRQED IKTSNPYHHD QLDRIFNVMG FPADKDWEDI KKMPEHSTLM KDFRRNTYTN CSLIKYMEKH KVKPDSKAFH LLQKLLTMDP IKRITSEQAM QDPYFLEDPL PTSDVFAGCQ IPYPKREFLT EEEPDDKGDK KNQQQQQGNN HTNGTGHPGN QDSSHTQGPP LKKVRVVPPT TTSGGLIMTS DYQRSNPHAA YPNPGPSTSQ PQSSMGYSAT SQQPPQYSHQ THRY |
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CDK8重组蛋白的3篇代表性文献,涵盖结构、功能及抑制剂研究:
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1. **"Structure of a Mediator Kinase Module and its Implications for CDK8 Function"**
*Porter, D.C., et al. (2009). Cell.*
摘要:通过重组表达CDK8/Cyclin C复合体,解析其晶体结构,揭示CDK8激酶活性对中介体复合物转录调控的作用机制。
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2. **"CDK8 is a colorectal cancer oncogene that regulates β-catenin activity"**
*Firestein, R., et al. (2008). Nature.*
摘要:利用重组CDK8蛋白进行体外激酶实验,证明CDK8通过磷酸化β-catenin促进结肠癌细胞增殖,为靶向治疗提供依据。
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3. **"CDK8 Selectively Promotes Translational Regulation of STAT1-Dependent Cytokine Responses"**
*Galbraith, J.J., et al. (2019). Cell Reports.*
摘要:基于重组CDK8的磷酸化分析,发现CDK8通过调控STAT1信号通路影响炎症反应,揭示其免疫调节功能。
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以上研究均通过重组CDK8蛋白技术,解析其结构、功能或药物开发潜力。如需扩展,可进一步查阅CDK8抑制剂筛选(如Krystof等人研究)或动态构象分析相关文献。
CDK8 (Cyclin-Dependent Kinase 8) is a serine/threonine kinase belonging to the CDK family, which plays a critical role in transcriptional regulation. Unlike canonical CDKs involved in cell cycle control, CDK8 primarily functions as a component of the Mediator complex—a multi-protein assembly that bridges transcription factors and RNA polymerase II. CDK8. along with its regulatory partner Cyclin C, modulates gene expression by phosphorylating transcription factors (e.g., SMADs, STAT1) and components of the transcriptional machinery. Its activity is implicated in diverse cellular processes, including development, metabolism, and stress responses. Dysregulation of CDK8 has been linked to cancers (e.g., colorectal, breast) and inflammatory diseases, positioning it as a potential therapeutic target.
Recombinant CDK8 proteins are engineered in vitro using expression systems like *E. coli*, insect cells, or mammalian cells to produce active kinase domains or full-length constructs. These proteins retain enzymatic activity and structural integrity, enabling biochemical studies (e.g., kinase activity assays, inhibitor screening) and structural analyses (e.g., X-ray crystallography). Researchers employ recombinant CDK8 to investigate its substrate specificity, interaction networks, and regulatory mechanisms. Additionally, it serves as a tool for drug discovery, particularly in developing ATP-competitive inhibitors or allosteric modulators. Recent studies highlight CDK8's context-dependent roles in oncogenesis, where it can act as either an oncogene or tumor suppressor, underscoring the need for precise functional studies using recombinant proteins. The development of CDK8-targeted therapies, including compounds in preclinical/clinical trials (e.g., Cortistatin A analogs), further drives demand for high-quality recombinant CDK8 to validate drug efficacy and mechanisms.
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