过渡性保护压力基因通过复合与铜进行点击反应
Suguru Yoshida1, Yasutomo Hatakeyama, Kohei Johmoto
1Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University , 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
Journal of the American Chemical Society
|September 19, 2014
概括
使用铜 (I) 盐暂时保护环素,使选择性点击化学成为可能. 这种方法允许在特定的基因位点进行受控的结合,使得循环基因衍生物在各种应用中更容易获得.
科学领域:
- 有机化学 有机化学
- 化学生物学 化学生物学
背景情况:
- 点击化学,特别是铜催化亚酸循环添加 (CuAAC),是分子构造的强大工具.
- 环节素是多功能构建块,但可以经历不必要的反应,限制它们的实用性.
研究的目的:
- 开发一个周期性菌素的过渡性保护策略,以防止过早反应.
- 为了使在其他反应性群体的存在下,能够选择性地功能化循环素.
主要方法:
- 复合的cyclooctynes与一个阴离子铜(I) 盐形成一个1: 1复合物,暂时掩盖的alkyne.
- 保护方法应用于带有终端基因分量的环素.
- 在未受保护的终端基中,选择性铜催化点击与化物的结合.
主要成果:
- 铜 (I) 复合物有效地阻止了循环环素与亚化物发生反应.
- 在受到保护的内部基因的存在下,在终端基因实现了选择性结合.
- 这一策略促进了复杂的cyclooctyne衍生物的合成.
结论:
- 已经建立了一种新型的周期性蛋白的短暂保护方法,使用铜 (I) 盐.
- 这种方法在点击化学中提供了直角控制,提高了功能化的环流素的可访问性.
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