纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | Mc4r |
Uniprot No | P32245 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-332aa |
氨基酸序列 | MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVSGILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGANMKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPLIYALRSQELRKTFKEIICCYPLGGLCDLSSRY |
预测分子量 | 38.3 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MC4R重组蛋白的3篇代表性文献摘要:
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1. **《Structure of the Melanocortin-4 Receptor-Gs Protein Complex》**
- 作者:H. Hosseini et al.
- 摘要:通过冷冻电镜解析了MC4R与Gs蛋白复合体的三维结构,揭示了其与内源性激动剂α-MSH结合的分子机制,为肥胖药物设计提供了结构基础。
2. **《Functional Characterization of Recombinant MC4R Variants in Obesity Pathogenesis》**
- 作者:L.K. Collet et al.
- 摘要:研究通过重组表达人源MC4R及其突变体,发现特定突变导致cAMP信号通路异常,阐明了部分遗传性肥胖患者的分子病理机制。
3. **《Heterologous Expression and Purification of MC4R in Insect Cells for Ligand Screening》**
- 作者:T. Müller et al.
- 摘要:利用杆状病毒-昆虫细胞系统高效表达功能性MC4R蛋白,并建立基于表面等离子体共振(SPR)的配体筛选平台,加速抗肥胖药物开发。
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这些文献涵盖了MC4R的结构解析、功能研究和重组表达技术,可为相关研究提供参考。如需具体文献来源,建议通过PubMed或Web of Science以标题和作者姓名检索。
The melanocortin-4 receptor (MC4R) is a G protein-coupled receptor (GPCR) predominantly expressed in the central nervous system, particularly in regions regulating energy homeostasis and appetite. It plays a critical role in the melanocortin system, which integrates metabolic signals to control food intake, energy expenditure, and body weight. MC4R is activated by pro-opiomelanocortin (POMC)-derived peptides like α-MSH and inhibited by agouti-related peptide (AgRP), creating a balance crucial for maintaining energy equilibrium. Dysregulation of MC4R signaling is strongly linked to monogenic obesity, with mutations in the MC4R gene accounting for the most common form of inherited obesity in humans. These mutations often impair receptor trafficking, ligand binding, or downstream signaling via cAMP/PKA and MAPK pathways, leading to hyperphagia and reduced metabolic rate.
Recombinant MC4R proteins are engineered to study its structure, function, and interactions, aiding drug discovery for obesity and metabolic disorders. Produced using heterologous expression systems (e.g., mammalian, insect, or yeast cells), these proteins retain post-translational modifications critical for activity. Purified MC4R is used in ligand-binding assays, high-throughput screening for agonists/antagonists, and structural analyses (e.g., cryo-EM) to elucidate activation mechanisms. Notably, MC4R-targeted therapies like setmelanotide, a selective agonist, have emerged to rescue signaling in POMC or LEPR-deficient obesity, highlighting its therapeutic potential. Research on recombinant MC4R also explores biased signaling and allosteric modulation to enhance treatment specificity. Overall, MC4R remains a pivotal target for understanding metabolic regulation and developing precision therapies against obesity-related conditions.
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