| 纯度 | >70%SDS-PAGE. |
| 种属 | Human |
| 靶点 | PDK1 |
| Uniprot No | Q15118 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 2-436aa |
| 氨基酸序列 | RLARLLRGA ALAGPGPGLR AAGFSRSFSS DSGSSPASER GVPGQVDFYA RFSPSPLSMK QFLDFGSVNA CEKTSFMFLR QELPVRLANI MKEISLLPDN LLRTPSVQLV QSWYIQSLQE LLDFKDKSAE DAKAIYDFTD TVIRIRNRHN DVIPTMAQGV IEYKESFGVD PVTSQNVQYF LDRFYMSRIS IRMLLNQHSL LFGGKGKGSP SHRKHIGSIN PNCNVLEVIK DGYENARRLC DLYYINSPEL ELEELNAKSP GQPIQVVYVP SHLYHMVFEL FKNAMRATME HHANRGVYPP IQVHVTLGNE DLTVKMSDRG GGVPLRKIDR LFNYMYSTAP RPRVETSRAV PLAGFGYGLP ISRLYAQYFQ GDLKLYSLEG YGTDAVIYIK ALSTDSIERL PVYNKAAWKH YNTNHEADDW CVPSREPKDM TTFRSA |
| 预测分子量 | 72 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3篇关于PDK1重组蛋白的经典文献概览：
1. **文献名称**：*Characterization of a 3-phosphoinositide-dependent protein kinase which phosphorylates and activates protein kinase Bα*
**作者**：Alessi DR, et al.
**摘要**：该研究首次在大肠杆菌中重组表达并纯化了PDK1蛋白，证实其通过磷酸化PKB/Akt激酶(Ser473位点)调控胰岛素信号通路，揭示了PDK1在细胞存活和代谢中的核心作用。
2. **文献名称**：*Crystal structure of the catalytic subunit of phosphoinositide-dependent kinase-1 (PDK1) in complex with a peptide inhibitor*
**作者**：Biondi RM, et al.
**摘要**：通过X射线晶体学解析了PDK1激酶结构域与抑制肽的复合物结构，阐明了其底物识别机制，为基于结构的抑制剂设计提供了关键依据。
3. **文献名称**：*Purification and characterization of recombinant human PDK1 expressed in Sf9 insect cells*
**作者**：Casamayor A, et al.
**摘要**：报道了利用杆状病毒-昆虫细胞系统高效表达人源PDK1重组蛋白，并优化纯化流程获得高活性蛋白，验证了其体外磷酸化下游底物SGK和PKCζ的能力。
**备注**：以上文献均发表于1997-2003年期间(如Alessi等1997年发表于*Current Biology*)，是PDK1功能与结构研究的奠基性工作。如需近年研究(如PDK1在癌症靶向治疗中的应用)，可补充说明获取更新文献。
Pyruvate dehydrogenase kinase 1 (PDK1) is a serine/threonine kinase that regulates cellular energy metabolism by phosphorylating and inhibiting the pyruvate dehydrogenase complex (PDC), a key enzyme linking glycolysis to the tricarboxylic acid (TCA) cycle. By controlling PDC activity, PDK1 modulates the flux of pyruvate into mitochondrial oxidative phosphorylation or its diversion toward lactate production, making it a critical regulator of metabolic flexibility. Dysregulation of PDK1 is implicated in metabolic disorders, cancer, and cardiovascular diseases, where aberrant glucose utilization supports pathological cell growth or survival.
Recombinant PDK1 protein is engineered using heterologous expression systems (e.g., E. coli, mammalian cells) to produce purified, functional kinase for research and drug discovery. Its recombinant form retains catalytic activity, enabling studies on substrate interactions, enzymatic kinetics, and inhibitor screening. Structural studies using recombinant PDK1 have revealed mechanisms of substrate recognition and allosteric regulation, particularly its interaction with the lipoyl domain of PDC.
Researchers employ recombinant PDK1 to explore its role in the Warburg effect—a metabolic shift favoring glycolysis in cancer cells—and to develop targeted therapies. Small-molecule inhibitors of PDK1. such as dichloroacetate (DCA), are investigated for their potential to restore mitochondrial respiration in cancer. Additionally, recombinant PDK1 aids in elucidating post-translational modifications (e.g., phosphorylation, acetylation) that modulate its activity under varying metabolic conditions. Quality-controlled batches ensure consistency in assays, supporting high-throughput screening and structural biology applications. This tool remains pivotal in advancing our understanding of metabolic reprogramming in disease and therapeutic intervention strategies.
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