循环图书馆成员的高通量序列确定通过部分埃德曼降解/质谱学
Sang Hoon Joo1, Qing Xiao, Yun Ling
1Department of Chemistry, The Ohio State University, 100 West 18th Avenue, Columbus, OH 43210, USA.
Journal of the American Chemical Society
|September 28, 2006
概括
一种新的高通量方法可以在药物发现中快速确定循环的序列. 这种技术简化了从生物医学研究的大型图书馆中识别有力的循环.
科学领域:
- 生物化学 生物化学
- 药用化学 医学化学
- 化学生物学 化学生物学
背景情况:
- 循环在药物发现和生物医学研究工具中非常有价值.
- 循环的组合图书馆是使用分割和池方法进行选的合成.
- 在选后确定击中周期性的序列一直是一个重大挑战.
研究的目的:
- 开发一种高通量方法来确定循环序列的成员.
- 克服在循环研究中对选后序列确定的局限性.
主要方法:
- 开发了一种使用具有空间分隔层的TentaGel微珠的新方法.
- 循环被显示在珠子表面,与编码线性在内核.
- 在内部编码上使用部分埃德曼降解/质谱实现了序列确定.
主要成果:
- 一个八类体库选确定了与斯特雷普塔维丁结合的循环.
- 一个类比库产生了具有增强抗菌活性的类比物.
- 该方法被证明是可靠的,简单的,快速的,和成本效益的循环序列的确定.
结论:
- 开发的方法显著提高了循环在生物医学研究中的实用性.
- 这种技术有助于识别和优化循环的药物发现和分子探针.
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