糖苷酶是广泛存在的酶，能催化寡糖和糖结合物中的糖苷键水解。这些酶在多种生物事件中起着重要作用，例如消化营养碳水化合物、溶酶体降解糖结合物和糖蛋白的翻译后修饰。异常的糖苷酶活性与多种疾病，尤其是癌症和溶酶体贮积病有关。鉴于糖苷酶的生理和病理重要性，开发针对这些酶的小分子化合物是糖科学和药物化学领域的热点研究。迄今为止进行的研究工作已经发现了很多靶向糖苷酶的小分子化合物，被用于阐明生物过程和开发有效的化疗药物。在本综述中，我们描述了2018年以来报道的研究结果，重点介绍了用于糖苷酶检测和成像的荧光探针、用于共价标记这些酶的活性探针、糖苷酶抑制剂和糖苷酶可活化前药。

Glycosidases are ubiquitous enzymes that catalyze the hydrolysis of glycosidic linkages in oligosaccharides and glycoconjugates. These enzymes play a vital role in a wide variety of biological events, such as digestion of nutritional carbohydrates, lysosomal catabolism of glycoconjugates, and posttranslational modifications of glycoproteins. Abnormal glycosidase activities are associated with a variety of diseases, particularly cancer and lysosomal storage disorders. Owing to the physiological and pathological significance of glycosidases, the development of small molecules that target these enzymes is an active area in glycoscience and medicinal chemistry. Research efforts carried out thus far have led to the discovery of numerous glycosidase-targeting small molecules that have been utilized to elucidate biological processes as well as to develop effective chemotherapeutic agents. In this review, we describe the results of research studies reported since 2018, giving particular emphasis to the use of fluorescent probes for detection and imaging of glycosidases, activity-based probes for covalent labelling of these enzymes, glycosidase inhibitors, and glycosidase-activatable prodrugs.