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在现场抑制剂合成和光极化选:加速药物发现的有效方法

Zhihong Li¹, Yue Wu¹, Shuai Zhen¹

¹State Key Laboratory of Natural Medicines Jiangsu Key Laboratory of Drug Design and Optimization, and Department of Chemistry China Pharmaceutical University Nanjing 211198 China.

Angewandte Chemie (Weinheim an der Bergstrasse, Germany)

|March 20, 2024

概括

在现场抑制剂合成和查 (ISISS) 通过结合合成和查,为药物发现提供了更简单的方法. 这种方法有效地确定了prolyl氧酶2 (PHD2) 的新型抑制剂,这是贫血治疗的关键标.

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:

针对目标的动态组合化学 (DCC) 对于命中鉴定有价值,但复杂的混合物分析阻碍了它的应用.
需要简化,高效的方法来识别命中和优化头.

研究的目的:

介绍并举例说明 in situ 抑制剂合成和选 (ISISS) 方法,作为 DCC.的可访问替代方法.
证明ISISS的实用性,用于发现针对治疗点的强效和新型抑制剂.

主要方法:

通过将高通量生物直角合成与基于光的合选开发ISISS.
结合光极化选与乙-化和化之间的反应.
应用ISISS来识别人类prolyl氧酶2 (PHD2) 的抑制剂.

主要成果:

通过使用ISISS方法成功识别了一种基于酸的强效和新型PHD2抑制剂.
发现的抑制剂在体内表现出与现有的已批准用于治疗贫血的药物相比具有相当的活力.
ISISS被证明是一个操作简单和高效的方法,用于击中发现.

结论:

ISISS提供了一种简化和有效的打击识别策略,克服了传统DCC的局限性.
这种方法有助于发现新型,强效的抑制剂,用于治疗标,如PHD2.2.
ISISS有望加速药物发现管道,特别是针对涉及贫血等疾病的目标.

关键词:

药物发现药物发现药物发现光的极化化光的极化氧气过低是因为缺氧.在现场的抑制剂合成和查.这是一个PHD2PHD2PHD2

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