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Updated: May 26, 2025

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将MIDA酸盐与含有脱氨酸的和蛋白质进行选择性合

Alexander A Vinogradov^1,2, Shih-Yu Pan¹, Hiroaki Suga¹

¹Department of Chemistry, Graduate School of Science, The University of Tokyo, Bunkyo-ku, Tokyo 113-0033, Japan.

Journal of the American Chemical Society

|February 21, 2025

概括

一种新的催化反应使和蛋白质中α,β-脱氨酸 (ΔAla) 的选择性晚期功能化成为可能. 这种方法具有很高的选择性,在温和的水性条件下进行,克服了现有技术的局限性.

科学领域:

生物化学
有机化学
化学生物学

背景情况:

α,β-脱氨酸 (ΔAla) 是一种用于修改,天然产品 (NP) 和蛋白质的反应性非蛋白质氨基酸.
目前的 ΔAla 修饰方法经常产生混合物,限制了它们在半合成工程和蛋白质突变发生中的应用.

研究的目的:

开发一种高度选择性的方法,用于和蛋白质中Dala的后期功能化.
克服现有技术的局限性,产生不良的产品混合物.

主要方法:

一种用介导的合反应,使用酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸酸.
使用N,N'-乙烯-bis-L作为Pd (II) 联体来增强反应速度和选择性.
应用该方法来功能化寡,NP类化合物和完整的蛋白质,包括体外翻译.

主要成果:

从含有 ΔAla 的和蛋白质中获得 ΔzPhe 的高度选择性合成.
在37°C的水中,反应在24小时内有效地进行,不需要排除氧气或基板保护.
证明了多种生物分子的成功功能化和化学基因组合成的适应.

结论:

开发了一种强大而选择性的Pd(II) 催化方法,用于后期的ΔAla功能化.
反应条件温和,多功能,适用于未受保护的基质,包括完整的蛋白质.
这种化学结构为和蛋白质工程以及新生物分子结构的合成提供了宝贵的工具.

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