中文摘要：

糖缀合物末端的唾液酸化修饰参与了很多重要的生理及病理过程，尤其是肿瘤细胞表面唾液酸过度表达，能够通过多种途径和机制促进肿瘤转移。唾液酸转移酶是人体内负责唾液酸化修饰的合成酶，良好的唾液酸转移酶抑制剂不仅能够充当糖生物学研究的探针分子，而且有望成为临床治疗中亟需的抑制肿瘤转移的药物。本文综述了近年来唾液酸转移酶抑制剂设计及发现的研究进展，重点介绍了不同类型抑制剂的设计思路及构效关系。此外，对该研究领域当前面临的一些挑战进行了探讨，并对其发展趋势进行了展望。

英文摘要：

Sialylation at the non-reducing end of glycoconjugates is involved in lots of important physiological and pathological processes. Especially cancer cells express high density of sialic acids known as hypersialylation that contributes to cancer cell progression and metastasis. Sialyltransferase is the glycosyltransferase in charge of sialylation of glycoconjugates. Effective sialyltransferase inhibitors could be not only of medicinal interests, especially in the therapy of cancer diseases, but also biological probes for studying fuctions of sialylation in glycobiology. Here we review recent progress of design and discovery of sialyltransferase inhibitors. The major content is about the design of different types of inhibitors and their structure-activity relationship. The current challenges and development trends are also proposed.