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Microarrays of tagged combinatorial triazine libraries in the discovery of small-molecule ligands of human IgG

机译:标记的组合三嗪文库的微阵列在人IgG小分子配体的发现中

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摘要

A novel and highly diverse tagged triazine library incorporating a triethylene glycol-based linker was synthesized using an orthogonal combinatorial approach on the solid phase and covalently immobilized on a glass substrate as a small molecule microarray (SMM). The SMM was screened with a fluorophore-conjugated human IgG, and 4 novel binders from a library of 2688 compounds were identified from the fully spatially addressable array without the need for compound decoding. Using surface plasmon resonance (SPR) analysis, binding seen on the array was confirmed, and a binding constant as low as K-d = 2.02 x 10(-6) M was measured.
机译:使用正交组合方法在固相上合成了一种新型且高度多样化的标签化三嗪文库,该文库结合了三甘醇基接头,并作为小分子微阵列(SMM)共价固定在玻璃基板上。用荧光团偶联的人IgG筛选SMM,无需完全解码化合物,即可从完全空间可寻址的阵列中鉴定出2688种化合物文库中的4种新型结合剂。使用表面等离振子共振(SPR)分析,确认在阵列上可见结合,并且测定的结合常数低至K-d = 2.02 x 10(-6)M。

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