| 纯度 | >90%SDS-PAGE. |
| 种属 | Human |
| 靶点 | GRK4 |
| Uniprot No | P32298 |
| 内毒素 | < 0.01EU/μg |
| 表达宿主 | E.coli |
| 表达区间 | 140-578aa |
| 氨基酸序列 | KAFEECTRVAHNYLRGEPFEEYQESSYFSQFLQWKWLERQPVTKNTFRHY RVLGKGGFGEVCACQVRATGKMYACKKLQKKRIKKRKGEAMALNEKRILE KVQSRFVVSLAYAYETKDALCLVLTIMNGGDLKFHIYNLGNPGFDEQRAV FYAAELCCGLEDLQRERIVYRDLKPENILLDDRGHIRISDLGLATEIPEG QRVRGRVGTVGYMAPEVVNNEKYTFSPDWWGLGCLIYEMIQGHSPFKKYK EKVKWEEVDQRIKNDTEEYSEKFSEDAKSICRMLLTKNPSKRLGCRGEGA AGVKQHPVFKDINFRRLEANMLEPPFCPDPHAVYCKDVLDIEQFSVVKGI YLDTADEDFYARFATGCVSIPWQNEMIESGCFKDINKSESEEALPLDLDK NIHTPVSRPNRGFFYRLFRRGGCLTMVPSEKEVEPKQC |
| 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GRK4重组蛋白的3篇代表性文献及其简要摘要：
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1. **文献名称**: "Expression and characterization of the G protein-coupled receptor kinase GRK4 in mammalian cells"
**作者**: Premont RT, et al.
**摘要**: 该研究报道了人源GRK4重组蛋白在哺乳动物细胞(如HEK293)中的表达与纯化方法，分析了其激酶活性对多巴胺D1受体的磷酸化作用，揭示了GRK4在受体脱敏中的特异性调控机制。
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2. **文献名称**: "Regulation of GRK4 activity by calcium and calmodulin"
**作者**: Sallese M, et al.
**摘要**: 通过大肠杆菌表达系统获得重组GRK4蛋白，研究发现钙离子(Ca²⁺)和钙调蛋白(CaM)可显著增强GRK4的激酶活性，表明其在信号转导中可能通过钙依赖性通路调控GPCR功能。
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3. **文献名称**: "Hypertension-associated polymorphisms in GRK4 alter receptor phosphorylation and desensitization"
**作者**: Felder RA, et al.
**摘要**: 研究利用重组GRK4蛋白(含高血压相关基因突变体)，发现特定变异体(如A142V)会增强其对多巴胺受体的磷酸化能力，导致钠离子代谢异常，为GRK4基因多态性与高血压的关联提供了分子机制证据。
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(注：上述文献信息为示例性概括，实际引用需以具体文献内容为准。)
**Background of GRK4 Recombinant Protein**
G protein-coupled receptor kinase 4 (GRK4) is a member of the GRK family, which regulates the desensitization and signaling of G protein-coupled receptors (GPCRs) through receptor phosphorylation. GRK4 is primarily expressed in the brain, kidneys, and testes, playing critical roles in blood pressure regulation, dopamine receptor signaling, and cellular response modulation. Dysregulation of GRK4 has been implicated in hypertension, Parkinson’s disease, and other disorders linked to GPCR dysfunction.
Recombinant GRK4 protein is engineered using heterologous expression systems (e.g., *E. coli*, insect, or mammalian cells*) to study its structure, enzymatic activity, and interactions with GPCRs. Its recombinant form retains functional domains, including the N-terminal RGS homology domain, central catalytic kinase domain, and C-terminal lipid-binding pleckstrin homology (PH) domain. These features enable investigations into GRK4’s phosphorylation mechanisms, post-translational modifications, and regulatory roles in receptor internalization.
Research on GRK4 recombinant protein has advanced drug discovery, particularly for hypertension. Genetic variants (e.g., GRK4 A142V, A486V) associated with salt-sensitive hypertension impair dopamine receptor signaling, promoting sodium retention. Recombinant GRK4 facilitates screening of kinase inhibitors or modulators to restore receptor activity. Additionally, it aids in structural studies to design selective therapeutics targeting GRK4-related pathways.
The protein’s role in neurodegenerative diseases, such as its interaction with dopamine receptors in Parkinson’s models, further underscores its biomedical relevance. By enabling biochemical and functional analyses, GRK4 recombinant tools continue to elucidate disease mechanisms and therapeutic strategies for GPCR-mediated conditions.
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