BMG多功能酶标仪国内用户出版物快报 (2025年6月)

>>>Self-assembling dendrimer nanodrug formulations for decreased hERG-related toxicity and enhanced therapeutic efficacy

国家纳米科学技术中心，中国科学院纳米材料生物医学效应与纳米安全重点实验室和重庆大学药学院天然产物合成与药物研究重庆市重点实验室的研究团队联合在专业学术期刊Science Advances上发表题为Self-assembling dendrimer nanodrug formulations for decreased hERG-related toxicity and enhanced therapeutic efficacy的研究文章，采用纳米技术应用于药物递送，以降低药物毒性和提高疗效，并将此技术用于研究hERG相关的心脏毒性。他们报道了使用自组装树状大分子纳米系统进行药物配制和递送，有效地降低了 hERG 结合和相关毒性，同时促进了治疗效果。这些树突纳米系统有效地封装了抗疟药氯喹、抗癌药阿霉素和 NUPR1 抑制剂 ZZW115，这三者都对 hERG 通道具有高亲和力。这些纳米制剂显示 hERG 结合亲和力降低了 3 到 8 倍，此研究强调了纳米技术在降低 hERG 结合和相关毒性的同时提高药物疗效的潜力，为药物开发提供了有价值的前景。                                          

研究团队使用 Predictor hERG 荧光偏振测定法对 hERG 钾通道阻滞电位进行评估，采用BMG的PHERAstar FSX多功能酶标仪，使用540和 573nm 的激发和发射波长下测量荧光偏振，进行hERG 通道结合试验。德国BMG的PHERAstar FSX专为高通量药物筛选设计，对于荧光偏振分子间相互作用实验所需要的双发射波长能在保证检测灵敏的前提下，同时检测平行和垂直方向的荧光信号，确保检测的准确性以及节省检测时间。仪器配置2对优化配对检测器，在TR-FRET，FP，BRET,FRET等同时双发射实验既有高的检测灵敏度又大大缩短检测时间，最高可适用到3456孔板，是高通量药物筛选的强大工具。

（原文：https://www.science.org/doi/10.1126/sciadv.adu9948）

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