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从庞大的图书馆中无条形码的成功发现,由自动化小分子结构注释启用

Edith van der Nol^1,2, Nils Alexander Haupt³, Qing Qing Gao¹

¹LACDR, Leiden University, Leiden, The Netherlands.

Nature communications

|October 28, 2025

概括

一个新的自编码库 (SEL) 平台允许在没有DNA标签的情况下选数百万个分子. 这种药物发现工具可以识别FEN1等具有挑战性的目标的强有力的结合剂,从而推进早期研究.

科学领域:

药用化学医学化学
生物化学生物化学
药物发现技术药物发现技术

背景情况:

亲和选择平台对于早期药物发现至关重要.
当前的DNA编码库 (DEL) 在合成和目标兼容性方面面临限制.

研究的目的:

引入一种新的无条码自编码库 (SEL) 平台,用于高通量选.
克服现有技术的局限性,特别是对于核酸结合点.

主要方法:

开发SELs,可以直接选超过50万个小分子.
整合双重质谱与自动结构注释定制软件的整合.
为各种化学架构建立高效,高多样性的合成协议.

主要成果:

针对碳酸无水酶IX的成功亲和性选择选,识别了多个纳米分子结合剂.
发现了DNA处理酶内核酶1 (FEN1) 的强效抑制剂.
展示SEL在一个实验中选大型图书馆的能力.

结论:

SEL平台提供了一个强大的,无标签的替代方案,用于选大型化学库.
这项技术将药物发现能力扩展到包括DNA处理酶在内的新目标类别.
对于学术和工业早期药物发现工作来说,SELs代表了重大进步.

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