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通过DELs,可以开发BRET探针,用于在细胞中进行目标参与研究

Kelly A Teske¹, Wenji Su², Cesear R Corona³

¹Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA.

Cell chemical biology

|July 25, 2023

概括

DNA编码图书馆 (DEL) 为药物发现提供了巨大的化学多样性. 这项研究证明了将DEL连接物转化为BRET探针用于活细胞向参与,加速药物开发.

科学领域:

药用化学医学化学
化学生物学化学生物学
药物发现药物发现药物发现

背景情况:

DNA编码图书馆 (DEL) 是发现新药线索的强大工具,因为它们具有巨大的化学多样性.
活细胞向参与研究对于在开发过程的早期验证候选药物至关重要.

研究的目的:

开发一种工作流程,用于从DEL联体生成BRET探针,用于活细胞向参与研究.
用极光酶A作为目标建立概念证明.
评估现有的DEL屏幕数据用于BRET探测器开发的重新用途.

主要方法:

利用双功能DEL连接体来创建BRET探测器.
进行了针对极光酶A的DEL屏幕.
将已识别的DEL配体转化为细胞活性BRET探针.
使用BRET探针验证和分层化学序列.

主要成果:

成功地将DEL连接物转化为细胞活性BRET探针用于极光激酶A.
证明了BRET探针在验证和分层DEL屏幕中的化学序列中的实用性.
展示了用于BRET探测器生成的先前存在的DEL屏幕数据的有效重新定位.

结论:

开发的DEL工作流有效地产生细胞活性BRET探针,独立于化合物结构或结构-活性关系 (SAR).
集成DEL和BRET技术显著加快了活细胞环境中的成功研究.

关键词:

在这里,我们可以看到AuroraAuroraAurora.这就是BRD4D.布雷特·布雷特是什么意思在这里,我们可以看到DEL DEL DEL DEL.一个DNA编码的图书馆.标签: 标签: IDO1 标签: IDO1 标签: IDO1 在NanoBRET中使用NanoBRET.在NanoLuc中使用NanoLuc.在Nlucc中使用.目标参与度目标参与度

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