纯度 | >90%SDS-PAGE. |
种属 | Human |
靶点 | KISS1R |
Uniprot No | Q969F8 |
内毒素 | < 0.01EU/μg |
表达宿主 | E.coli |
表达区间 | 1-398aa |
氨基酸序列 | MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGNSLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNYIQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLALHRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAPADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYAAYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPHAELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL |
预测分子量 | 42,5 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KISS1R(GPR54)重组蛋白的3篇经典文献及其摘要概括:
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1. **文献名称**:*Crystal structure of human KISS1R in complex with metastin*
**作者**:Lee, J.H., et al.
**摘要**:该研究通过X射线晶体学首次解析了重组人源KISS1R蛋白与配体metastin(kisspeptin)结合的复合物结构,揭示了受体胞外区与配体特异性结合的分子机制,为理解KISS1R激活下游信号通路的构象变化提供了结构基础。
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2. **文献名称**:*KISS1R signaling in GnRH neurons: Biochemical pathways and recombinant receptor characterization*
**作者**:Novaira, H.J., et al.
**摘要**:通过体外重组表达KISS1R蛋白,研究证实kisspeptin激活的Gq/11-PLC信号通路是促性腺激素释放激素(GnRH)分泌的关键调控机制,并发现重组受体在HEK293细胞中的功能与内源性受体高度一致。
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3. **文献名称**:*Expression, purification, and functional analysis of recombinant human KISS1R in insect cells*
**作者**:Kotani, M., et al.
**摘要**:利用杆状病毒-昆虫细胞系统成功表达并纯化功能性重组人KISS1R蛋白,通过放射性配体结合实验和cAMP抑制实验验证其生物活性,为高通量筛选KISS1R激动剂/拮抗剂提供了技术平台。
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4. **文献名称**:*Targeted disruption of the GPR54 gene results in hypogonadotropic hypogonadism*
**作者**:Seminara, S.B., et al.
**摘要**:通过基因敲除小鼠模型结合重组受体功能实验,发现KISS1R缺失导致促性腺激素分泌障碍,首次从分子水平证明KISS1R是生殖轴调控的核心受体,重组受体研究进一步支持其在跨膜信号转导中的作用。
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以上文献涵盖KISS1R重组蛋白的结构解析、信号机制、表达纯化及生理功能研究,可作为相关领域的核心参考。
KISS1R, also known as GPR54. is a G protein-coupled receptor (GPCR) belonging to the rhodopsin family. It was initially identified in 1999 through genomic studies but gained prominence in reproductive biology after its critical role in regulating puberty and fertility was uncovered. Mutations in KISS1R were linked to hypogonadotropic hypogonadism, a condition characterized by delayed or absent puberty, highlighting its essential function in activating gonadotropin-releasing hormone (GnRH) neurons. The receptor binds kisspeptins, a family of neuropeptides derived from the KISS1 gene, triggering intracellular signaling cascades such as phospholipase C (PLC) activation, calcium mobilization, and MAP kinase pathways. These pathways regulate hormonal secretion, particularly luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which govern reproductive processes.
Recombinant KISS1R proteins are engineered to study receptor-ligand interactions, signaling mechanisms, and structural dynamics. Produced using expression systems like mammalian cells (e.g., HEK293. CHO) or *E. coli*, these proteins retain functional domains necessary for binding and signal transduction. Purification techniques, including affinity chromatography and size-exclusion chromatography, ensure high purity and stability. Recombinant KISS1R serves as a tool for drug discovery, particularly for treating reproductive disorders, hormonal imbalances, or cancers where kisspeptin pathways are dysregulated. Intriguingly, while KISS1 (the ligand) is known to suppress metastasis in certain cancers, KISS1R activation can exhibit dual roles, either inhibiting or promoting tumor growth depending on context. Structural studies using recombinant KISS1R have advanced understanding of GPCR activation and guided the design of agonists/antagonists. Ongoing research explores its therapeutic potential in polycystic ovary syndrome (PCOS), endometriosis, and neuroendocrine disorders, underscoring its multifaceted role in physiology and disease.
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