BMG多功能酶标仪国内用户出版物快报 (2025年4月)

>>>Rational Design Biased Compounds against μ-Opioid Receptor

中国科学院深圳先进技术研究院计算机辅助药物发现研究中心和深圳阿尔法分子科技有限责任公司的研究团队联合在专业学术期刊ACS Pharmacology & Translational Science上发表题为Rational Design Biased Compounds against μ-Opioid Receptor的研究文章，研究靶向 μ-阿pian受体 （MOR） 的激动剂的镇痛药，μ-阿pian受体的激动剂因其临床使用受到不良副作用的限制，这些副作用部分是由 β-arrestin 信号诱导的。科研人员将计算机方法和基于细胞的功能测定相结合，设计了具有高亲和力的新型结构支架分子，这些分子偏向 MOR 的 G 蛋白信号传导。为配体-MOR 结合模式提供了深刻的见解，可以作为设计副作用减少的下一代 MOR 配体的重要指南。                                        

研究团队采用BMG的PHERAstar FSX多功能酶标仪进行基于BRET的cAMP检测。德国BMG的PHERAstar FSX专为高通量药物筛选设计，对于BRET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2个不同发射波长的信号，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。

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Rational Design Biased Compounds against μ-Opioid Receptor

中国科学院深圳先进技术研究院计算机辅助药物发现研究中心

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