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Updated: Jul 26, 2025

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Published on: August 1, 2018

酸-高价反应剂奇默体:使酸功能化和宏循环化成为可能

Xing-Yu Liu¹, Xinjian Ji², Christian Heinis²

¹Laboratory of Catalysis and Organic Synthesis, Ecole Polytechnique Fédérale de Lausanne, EPFL, 1015, Lausanne, Switzerland.

Angewandte Chemie (International ed. in English)

|June 13, 2023

概括

这项研究引入了用于改的乙烯二醇 (EBX),使有效的合和宏循环形成成为可能. 这些新型EBX在化学生物学和药物发现中提供了多方面的应用.

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科学领域:

有机化学有机化学
化学生物学化学生物学
药用化学医学化学

背景情况:

的修饰对于开发新疗法和化学探针至关重要.
现有的联和宏循环化方法在范围和效率上可能受到限制.

研究的目的:

开发一种新的策略,用于使用乙烯基二醇 (EBXs) 进行基修饰.
探索EBXs在联和光催化大循环中的实用性.
为了研究改性作为蛋白质-蛋白质相互作用抑制剂的潜力.

主要方法:

通过溶液和固体相合成 (SPPS) 合成乙烯基二醇 (-EBXs).
在有机溶剂和水性缓冲器中与氨酸残留物发生合反应.
用于分子内宏循环的光催化脱碳化合.
设计和合成一个刚性线性arylalkyne链接器.

主要成果:

成功合成了-EBX,并证明了多功能反应性.
通过与氨酸的反应实现了有效的-和-蛋白合.
一种新的光催化方法使分子内宏循环化成为可能,形成循环.
一种特定的链结合物在Nrf2结合部位对Keap1具有很高的亲和力.

关键词:

超价反应剂超价反应剂 Keap1-Nrf2 蛋白质与蛋白质相互作用抑制剂.的宏循环化的宏循环化类/蛋白质修饰类/蛋白质修饰

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相关实验视频

Last Updated: Jul 26, 2025

Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation

Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation

Published on: August 1, 2018

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Published on: September 28, 2022

Targeted Antibody Blocking by a Dual-Functional Conjugate of Antigenic Peptide and Fc-III Mimetics DCAF

Targeted Antibody Blocking by a Dual-Functional Conjugate of Antigenic Peptide and Fc-III Mimetics DCAF

Published on: September 17, 2019

结论:

乙烯基二多索隆为基修饰和结合提供了一种强大的新工具.
开发的方法允许有效合成线性和宏循环.
这些发现为设计基于的蛋白质蛋白相互作用抑制剂开辟了道路,例如涉及Nrf2和Keap1.1的蛋白质蛋白相互作用抑制剂.