在微型板中合成糖阵列
Fabio Fazio1, Marian C Bryan, Ola Blixt
1Department of Chemistry and Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
Journal of the American Chemical Society
|November 28, 2002
概括
这项研究展示了一种新的方法,利用点击化学在微型板上合成复杂的碳水化合物阵列. 这些阵列能够有效地选莱克相互作用和重要甘氨酸的酶合成,如sialyl Lewis x.
科学领域:
- 碳水化合物化学 碳水化合物化学
- 葡萄糖生物学 葡萄糖生物学
- 化学生物学 化学生物学
背景情况:
- 氧化糖的合成和显示对于理解碳水化合物-蛋白质相互作用至关重要.
- 基于microtiter板的测试为生物查提供了一个高通量平台.
研究的目的:
- 开发一种合成和显示复杂碳水化合物阵列在微型板表面的方法.
- 为了利用这些数组进行莱克查和酶合成甘氨酸.
主要方法:
- 使用1,3-双极循环添加剂 (点击化学) 来将寡糖类固定到C(14) 碳化合物链上.
- 在微板中进行微分子尺度上糖阵列的现场合成.
- 使用ESI-MS确认产品形成,并通过化学和生物测试确定产量.
主要成果:
- 在微型板上成功合成并显示各种复杂碳水化合物 (6-16).
- 证明了这些阵列的高效选与不同的lectins.
- 通过板显示前体的fucosylation实现了sialyl Lewis x (17) 的酶合成.
- 对于抑制剂20所获得的IC(50) 值与溶液阶段研究一致.
结论:
- 开发的方法提供了一个多功能平台,用于在微型板中生成碳水化合物阵列.
- 这种方法有助于高通量选碳水化合物-莱克相互作用.
- 在固体支上合成复杂甘氨酸的酶是可行的和高效的.
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