基于D-半乳糖衍生的小分子半乳糖凝集素抑制剂的合成及活性研究进展

Research Progress on the Synthesis and Activity of D-Galactose Derived Small Galectin Inhibitors

半乳糖凝集素是一类能够特异性识别β-半乳糖苷结构的可溶性蛋白,广泛分布于正常组织和病变组织中,在细胞黏附、细胞凋亡、炎症反应和肿瘤转移等过程具有重要作用,是治疗肿瘤、炎症及神经性疾病等多种疾病的潜在靶点.根据衍生位点的差异,按照半乳糖单取代、双取代和多取代衍生物的顺序对近十多年来基于D-半乳糖衍生的小分子半乳糖凝集素抑制剂进行分类,总结了这些抑制剂的化学合成方法及活性研究进展,期望能为高活性和高选择性的半乳糖凝集素抑制剂的设计提供思路,为靶向半乳糖凝集素的新型药物开发提供参考.

Galectins are a family of soluble proteins which can specifically recognize the structure ofβ-galactoside.It is widely distributed in normal and diseased tissues,and plays an important role in cell adhesion,cell apoptosis,inflammatory response,tumor metastasis and other related processes.Galectin is a promising target for the treatment of many diseases,such as tumor,inflammation and neurological diseases.Herein,the synthesis and biological activities of small galectin inhibitors derived from D-galactose are reviewed according to the difference of derivatization sites,which are expected to provide research thought for designing galectin inhibitors with high affinity and high selectivity,and afford reference for development of new drug candidates targeting galectins.