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显示混合折叠分子-质宏循环的选择

Sebastian Dengler¹, Ryan T Howard¹, Vasily Morozov¹

¹Department of Pharmacy and Center for Integrated Protein Science, Ludwig-Maximilians-Universität, Butenandtstr. 5-13, 81377, München, Germany.

Angewandte Chemie (International ed. in English)

|September 14, 2023

概括

研究人员通过结合芳香螺旋式折叠体,扩大了类宏循环库的化学多样性. 这使得能够选择结合目标蛋白质的混合宏循环,从而增强蛋白质识别策略.

科学领域:

生物化学生物化学
化学生物学化学生物学
结构生物学结构生物学

背景情况:

在类宏循环库中扩大化学多样性对于改善生物分子标结合至关重要.
目前的方法限制了可访问的化学空间,用于显示选择.

研究的目的:

为了将一个大型芳香螺旋式折叠器纳入类宏循环以进行显示选择.
为蛋白质识别选择和表征新的宏循环折叠分子-混合体.

主要方法:

能够进行柔性酶介导的tRNA化和核糖体翻译启动的折叠体的鉴定.
mRNA显示选择以识别宏循环折叠分子-混合体.
结晶结构的确定和分子动力学模拟.

主要成果:

为E6AP HECT域选择了一种具有纳米分子亲和力的混合宏环结合剂.
选择的混合体表现出高度融合的序列.
结构分析揭示了和折叠机组件之间的相互螺旋拼接.

结论:

加入芳香折叠剂显著扩大了用于显示器选择的化学空间.
折叠分子-混合物为蛋白质识别提供了一个有前途的策略,折叠分子稳定螺旋.
这种方法增强了类宏循环在治疗应用中的潜力.

关键词:

显示选择选择显示选择折机折机是一种折机.宏观循环是一种宏观循环.酸是一种酸.蛋白质识别功能蛋白质识别功能

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