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思维的转变:基于细胞热位移分析的药物发现

A Shift in Thinking: Cellular Thermal Shift Assay-Enabled Drug Discovery.

作者信息

Caballero Isabel Martín, Lundgren Stina

机构信息

Pelago Bioscience AB, 17165 Solna, Sweden.

出版信息

ACS Med Chem Lett. 2023 Mar 17;14(4):369-375. doi: 10.1021/acsmedchemlett.2c00545. eCollection 2023 Apr 13.

Abstract

A decade has passed since the cellular thermal shift assay (CETSA) was introduced to the drug discovery community. Over the years, the method has guided numerous projects by providing insights about, for example, target engagement, lead generation, target identification, lead optimization, and preclinical profiling. With this Microperspective, we intend to highlight recently published applications of CETSA and how the data generated can enable efficient decision-making and prioritization throughout the drug discovery and development value chain.

摘要

细胞热位移分析(CETSA)被引入药物研发领域已有十年。多年来,该方法通过提供有关靶点结合、先导化合物生成、靶点鉴定、先导化合物优化和临床前分析等方面的见解,指导了众多项目。通过这篇微观视角文章,我们旨在突出CETSA最近发表的应用,以及所生成的数据如何在整个药物研发和开发价值链中实现高效决策和优先级排序。

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