| 牛文嘉#,侯梦露#,高姗,等.基于KLHDC2配体的筛选模型的建立及应用研究[J].中国海洋药物,2026,(3):-. |
| 基于KLHDC2配体的筛选模型的建立及应用研究 |
| Development and Application of a Screening Model Based on KLHDC2 Ligands |
| 投稿时间：2025-03-13 修订日期：2025-04-23 |
| DOI： |
| 中文关键词: KLHDC2 FRET 亲和力 |
| English Keywords:KLHDC2, FRET, binding affinity |
| Fund Project: |
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| 中文摘要: |
| 目的 构建基于KLHDC2蛋白的FRET筛选模型,为靶向KLHDC2的药物筛选提供一种可靠的高通量检测方法。方法 构建pFastbac-6×His-GST-TEV-KLHDC2质粒,并利用杆状病毒表达系统感染昆虫细胞进行蛋白表达与纯化,并对其进行荧光标记,成功建立了FRET技术检测体系,用于评估化合物与KLHDC2蛋白的相互作用。结果 利用构建的KLHDC2蛋白FRET筛选模型进行化合物筛选,发现化合物K1与KLHDC2蛋白表现出显著的结合亲和力,其结合能力与阳性对照配体相当。结论 本研究成功构建基于KLHDC2蛋白的FRET筛选模型,为基于KLHDC2的药物筛选提供了灵敏、可靠的高通量检测平台。 |
| English Summary: |
| Objective To establish a FRET-based screening model targeting the KLHDC2 protein, providing a reliable high-throughput detection method for drug screening focused on the KLHDC2 target. Methods The pFastbac-6×His-GST-TEV-KLHDC2 plasmid was constructed, and the baculovirus expression system was utilized to infect insect cells for protein expression and purification. The purified protein was fluorescently labeled, successfully establishing a FRET-based detection system to evaluate the interaction between compounds and the KLHDC2 protein. Results Using the constructed KLHDC2 protein FRET screening model, compound K1 demonstrated significant binding affinity to the KLHDC2 protein, with its binding capability comparable to that of the positive control ligand. Conclusion This study successfully developed a FRET-based screening model for the KLHDC2 protein, offering a sensitive and reliable high-throughput detection platform for drug screening targeting KLHDC2. |
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