在温和的pH值下用碳化物进行化学选择性托芬标记
John M Antos1, Jesse M McFarland, Anthony T Iavarone
1Department of Chemistry, University of California, Berkeley, California 94720-1460, USA.
Journal of the American Chemical Society
|April 16, 2009
概括
研究人员使用水中的碳化物改进了一种托芬修饰方法. 这种新技术在pH 6-7下起作用,使和蛋白质能够通过可访问的托残留物进行修改.
科学领域:
- 有机化学 有机化学
- 生物化学 生物化学
- 化学生物学 化学生物学
背景情况:
- 在蛋白质研究中,托芬的修饰是至关重要的.
- 之前使用碳化的方法受到pH条件的限制.
- 需要适用于各种和蛋白质基质的可靠方法.
研究的目的:
- 为了改进现有的碳化物介导的水溶液中的酸修饰.
- 为了扩大pH值范围以实现高效的内醇修饰.
- 为了证明该方法在和蛋白质基板上的实用性.
主要方法:
- 使用N- ((tert-butyl) 胺,以促进与碳酸的醇修饰.
- 在广泛的pH范围 (2-7) 中,在水溶液中进行反应.
- 通过使用热变性化来研究溶剂可访问性的影响.
主要成果:
- 在水溶液中的pH 6-7时成功实现了托芬修饰.
- 证明了40-60%的转化产量,在和蛋白质上具有出色的托化学选择性.
- 确认了因多尔侧链的溶剂可访问性,因为它对碳化合物添加至关重要.
结论:
- 开发了一种改进的,广泛适用的水性托芬修饰方法.
- 该方法有效修改和蛋白质,特别是那些含有溶剂可访问的酸的蛋白质.
- 在工程蛋白质方面取得了进展,用于有针对性的修改,可访问的托.
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