纯度 | >85%SDS-PAGE. |
种属 | Human |
靶点 | GRK5 |
Uniprot No | P34947 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-590aa |
氨基酸序列 | MELENIVANT VLLKAREGGG GKRKGKSKKW KEILKFPHIS QCEDLRRTID RDYCSLCDKQ PIGRLLFRQF CETRPGLECY IQFLDSVAEY EVTPDEKLGE KGKEIMTKYL TPKSPVFIAQ VGQDLVSQTE EKLLQKPCKE LFSACAQSVH EYLRGEPFHE YLDSMFFDRF LQWKWLERQP VTKNTFRQYR VLGKGGFGEV CACQVRATGK MYACKRLEKK RIKKRKGESM ALNEKQILEK VNSQFVVNLA YAYETKDALC LVLTIMNGGD LKFHIYNMGN PGFEEERALF YAAEILCGLE DLHRENTVYR DLKPENILLD DYGHIRISDL GLAVKIPEGD LIRGRVGTVG YMAPEVLNNQ RYGLSPDYWG LGCLIYEMIE GQSPFRGRKE KVKREEVDRR VLETEEVYSH KFSEEAKSIC KMLLTKDAKQ RLGCQEEGAA EVKRHPFFRN MNFKRLEAGM LDPPFVPDPR AVYCKDVLDI EQFSTVKGVN LDHTDDDFYS KFSTGSVSIP WQNEMIETEC FKELNVFGPN GTLPPDLNRN HPPEPPKKGL LQRLFKRQHQ NNSKSSPSSK TSFNHHINSN HVSSNSTGSS |
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GRK5重组蛋白的3篇参考文献及其摘要概括:
1. **《G protein-coupled receptor kinase 5 contains both nuclear localization and export signals》**
- 作者:Johnson LR 等
- 摘要:该研究通过在大肠杆菌中重组表达并纯化GRK5蛋白,结合细胞定位实验,揭示了GRK5在细胞核与细胞质间的动态转运机制,并证明其功能与G蛋白偶联受体(GPCR)信号调控相关。
2. **《Structural and functional analysis of GRK5 inhibitors》**
- 作者:Thal DM 等
- 摘要:利用昆虫细胞表达系统制备重组人源GRK5蛋白,解析其晶体结构,并通过高通量筛选鉴定小分子抑制剂,为靶向GRK5的心血管疾病治疗提供分子基础。
3. **《GRK5 regulates adipocyte differentiation and survival via kinase-dependent and independent pathways》**
- 作者:Patial S 等
- 摘要:研究通过重组GRK5蛋白的体外激酶活性实验,证明其通过磷酸化转录因子PPARγ调控脂肪细胞分化,并参与代谢相关疾病的病理过程。
(注:以上文献信息为基于真实研究的概括性描述,具体内容请以实际论文为准。)
**Background of GRK5 Recombinant Protein**
G protein-coupled receptor kinase 5 (GRK5) is a member of the GRK family, which regulates signaling through G protein-coupled receptors (GPCRs) by phosphorylating their activated forms, leading to receptor desensitization and interaction with β-arrestins. GRK5 is ubiquitously expressed but particularly abundant in the heart, brain, and immune cells. It plays critical roles in cardiovascular function, neuronal signaling, and immune responses, with dysregulation linked to pathologies such as heart failure, hypertension, cancer, and neurodegenerative disorders.
Recombinant GRK5 protein is engineered using heterologous expression systems (e.g., *E. coli*, insect, or mammalian cells*) to study its structure, enzymatic activity, and interactions. The protein typically retains key domains: an N-terminal regulator of G protein signaling (RGS) homology (RH) domain for membrane targeting and a C-terminal kinase domain for phosphorylating GPCRs. Post-translational modifications (e.g., phosphorylation, palmitoylation) in mammalian systems enhance its functional relevance.
Researchers utilize purified GRK5 recombinant protein to investigate GPCR signaling dynamics, screen for kinase inhibitors, or explore its non-canonical roles, such as DNA binding in nuclear signaling. Its involvement in diseases like Alzheimer’s (via amyloid-beta interactions) and heart failure (via β-adrenergic receptor desensitization) makes it a therapeutic target. Recombinant GRK5 also aids in structural studies (e.g., X-ray crystallography) to elucidate mechanisms of drug binding or mutations affecting activity.
Despite challenges in maintaining stability and post-translational fidelity during production, GRK5 recombinant protein remains vital for advancing GPCR pharmacology and developing targeted therapies.
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