Synthesis, decoding, and preliminary screening of a bead-supported split-pool library of triboronic acid receptors for complex oligosaccharides

Synthesis, decoding, and preliminary screening of a bead-supported split-pool library of triboronic acid receptors for complex oligosaccharides
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DOI:
10.1071/ch07263
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发表时间:
2007-01-01
影响因子:
1.1
通讯作者:
Hall, Dennis G.
Hall, Dennis G.
中科院分区:
化学4区
文献类型:
--
作者:
Manku, Sukhdev;Hall, Dennis G.

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采用珠子编码的裂解池策略,通过部分末端合成的方法,实现了289个三胺三硼酸低聚糖受体原型的珠状支持组合文库的可控合成。尽管在中性水中针对Lewis-b四糖的初步筛选未能显示紧密结合的受体,但使用高效液相色谱-电喷雾质谱仪检测可以有效地解码文库中的单个珠子。在改进的糖苷结合的硼酸单元的帮助下,这一概念验证可以变得普遍适用。
A controlled synthesis of a prototypic bead-supported combinatorial library of 289 triamine-derived triboronic acid receptors for oligosaccharides was achieved using the split-pool strategy with bead encoding using the method of partial termination synthesis. Although a preliminary screening of the library against the Lewis-b tetrasaccharide in neutral water failed to show tight-binding receptors, single beads from the library can be decoded efficiently using high performance liquid chromatography with electrospray mass spectrometric detection. This proof-of-concept could become generally applicable with the help of improved glycoside-binding boronic acid units.