| 基于DARTS技术的丹参素钠直接结合靶蛋白鉴定 |
| |
| 引用本文： | 陈缘静,蒋薇薇,李丽华,张成中,贾丹,张川.基于DARTS技术的丹参素钠直接结合靶蛋白鉴定[J].药学与临床研究,2022,30(1):58-61. |
| |
| 作者姓名： | 陈缘静 蒋薇薇 李丽华 张成中 贾丹 张川 |
| |
| 作者单位： | 海军军医大学 药学系,上海 200433,海军军医大学 药学系,上海 200433;上海大学 医学院,上海 200444 |
| |
| 基金项目： | 海军军医大学本科创新孵化基地项目（PH2019104） |
| |
| 摘 要： | 目的：鉴定丹参素钠在人脐静脉内皮细胞中可能直接结合的靶蛋白。方法：首先利用药物亲和反应靶点稳定技术（DARTS），结合聚丙烯酰胺凝胶电泳（SDS-PAGE）及基质辅助激光解吸电离飞行时间串联质谱（MALDI-TOF/TOF-MS）鉴定丹参素钠在人脐静脉内皮细胞（HUVEC）中可能直接结合的靶蛋白，并通过免疫印迹法（Western blotting）进行验证。然后采用表面等离子共振技术（SPR）分析丹参素钠与其潜在靶标蛋白的结合动力学参数。结果：丹参素钠在HUVEC细胞中特异性结合CD44蛋白，两者之间的结合常数为4.84×10-4 mol·L-1。结论：丹参素钠可能通过结合靶蛋白CD44发挥心血管的保护作用。
|
| 关 键 词： | 丹参素钠 药物亲和反应靶点稳定技术 CD44 表面等离子共振 |
| 收稿时间： | 2021/4/14 0:00:00 |
| 修稿时间： | 2022/2/13 0:00:00 |
Target Identification of Sodium Danshensuusing Drug Affinity Responsive Target Stability Technique |
| |
| Chenyuanjing,Jiangweiwei,Lilihu,Zhangchengzhong,Jiadan and Zhangchuan.Target Identification of Sodium Danshensuusing Drug Affinity Responsive Target Stability Technique[J].Pharmacertical and Clinical Research,2022,30(1):58-61. |
| |
| Authors: | Chenyuanjing Jiangweiwei Lilihu Zhangchengzhong Jiadan and Zhangchuan |
| |
| Institution: | Naval Medical University,Naval Medical University,Naval Medical University,Naval Medical University,Naval Medical University,Naval Medical University |
| |
| Abstract: | Objective: To identify the direct binding protein(s) of sodium Danshensu in human umbilical vein endothelial cells. Methods: Drug affinity responsive target stability (DARTS) technique combined with SDS-PAGE and MALDI-TOF/TOF-MS were applied to identify the direct binding proteins of sodium Danshensu in human umbilical vein endothelial cells, which was verified by western blotting. Moreover, surface plasmon resonance(SPR) was performed to identify the binding mode of sodium Danshensu and its target protein. Results: Sodium Danshensu specially bound to CD44 with a KD value of 4.84 × 10-4 mol·L-1. Conclusion: Sodium Danshensumay exert its cardioprotectiveeffects by targeting CD44. |
| |
| Keywords: | Sodium Danshensu Drug affinity responsive target stability technique CD44 Surface plasmon resonance technology |
| 本文献已被 万方数据 等数据库收录！ |
| 点击此处可从《药学与临床研究》浏览原始摘要信息 |
| 点击此处可从《药学与临床研究》下载免费的PDF全文 |
