Liang R, Yan L, Loebach J, Ge M, Uozumi Y, Sekanina K, Horan N, Gildersleeve J, Thompson C, Smith A, Biswas K, Still W C, Kahne D
Department of Chemistry, Princeton University, Princeton, NJ 08544, USA.
Science. 1996 Nov 29;274(5292):1520-2. doi: 10.1126/science.274.5292.1520.
A solid phase carbohydrate library was synthesized and screened against Bauhinia purpurea lectin. The library, which contains approximately 1300 di- and trisaccharides, was synthesized with chemical encoding on TentaGel resin so that each bead contained a single carbohydrate. Two ligands that bind more tightly to the lectin than Gal-beta-1,3-GalNAc (the known ligand) have been identified. The strategy outlined can be used to identify carbohydrate-based ligands for any receptor; however, because the derivatized beads mimic the polyvalent presentation of cell surface carbohydrates, the screen may prove especially valuable for discovering new compounds that bind to proteins participating in cell adhesion.
合成了一个固相碳水化合物文库,并针对紫羊蹄甲凝集素进行筛选。该文库包含约1300种二糖和三糖,在TentaGel树脂上进行化学编码合成,使得每个珠子都含有一种单一的碳水化合物。已鉴定出两种比已知配体Gal-β-1,3-GalNAc与凝集素结合更紧密的配体。所述策略可用于鉴定任何受体的基于碳水化合物的配体;然而,由于衍生化的珠子模拟了细胞表面碳水化合物的多价呈现,该筛选对于发现与参与细胞黏附的蛋白质结合的新化合物可能特别有价值。