BMG多功能酶标仪国内用户出版物快报 (2024年5月)

>>>Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2

百济神州(北京)有限公司药物化学研究室在专业学术期刊Journal of Medicinal Chemistry发表了题为Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2的文章，研究B细胞淋巴瘤-2（Bcl-2）选择性抑制剂，用于治疗慢性淋巴细胞白血病。科学家们做了全面的结构优化产生了临床候选BGB-11417（化合物12e，sonrotoclax），其对WT Bcl-2和G101V突变体都表现出强烈的体外和体内抑制活性，并且对Bcl-xL表现出优异的选择性，而没有明显的细胞色素P450抑制。目前，BGB-11417作为单一疗法和联合疗法正在接受II/III期临床评估。

科研工作者借助BMG的 PHERAstar FSX多功能酶标仪，借助TR-FRET检测技术来进行药物竞争性结合分析，将不同药物浓度下蛋白-配体相互作用的抑制百分比进行4参数拟合，计算每个化合物的IC50。BMG的 PHERAstar FSX多功能酶标仪硬件配置TR-FRET专用激光光源和专用的配对红敏检测器，在飞速读板的设置下依然能获得稳定的数据，是TR-FRET检测的有力工具。对于结合动力学实验，软件拥有专用的分析工具，轻松获取Ka，Kd值。PHERAstar FSX多功能酶标仪还配置配对的低噪音检测器，各种分子间相互作用实验均可轻松完成。

（原文：https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c00027）

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Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2

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