Tejler Johan, Salameh Bader, Leffler Hakon, Nilsson Ulf J
Organic Chemistry, Lund University, POB 124, SE-22100, Lund, Sweden.
Org Biomol Chem. 2009 Oct 7;7(19):3982-90. doi: 10.1039/b909091f. Epub 2009 Jul 20.
A fragment-based development of 3C-triazol-1-yl-O-galactopyranosyl aldoximes led to the discovery of highly selective and high affinity (K(d) down to 11 microm) small monosaccharide based inhibitors of galectin-3. Galectin-7, 8 N-terminal CRD, and 9 N-terminal CRD bound the inhibitors only weakly. The galectin-3 selectivity was hypothesized to stem from interaction of the aldoxime moiety with a site not present in the other galectins.
基于片段的3C-三唑-1-基-O-吡喃半乳糖醛肟的开发导致发现了高选择性和高亲和力（解离常数低至11微摩尔）的基于单糖的半乳糖凝集素-3小分子抑制剂。半乳糖凝集素-7、8的N端CRD和9的N端CRD与这些抑制剂的结合较弱。据推测，半乳糖凝集素-3的选择性源于醛肟部分与其他半乳糖凝集素中不存在的位点的相互作用。
