Sialic acid which often terminated in the carbohydrate chain of glycoconjugates, is closely related to organs development and various disease progression. Sialic acids may regulate the biological functions of glycoconjugates through removing the sialic acid on them and changing their conformation. Up to date, four sialidases have been found in mammalian cells, and the research on sialidase 1 (Neu1)is more widely. The hydrolysis substrates of Neu1 are varied, and strongly linked to the structure and function of cell surface receptors. Recent evidence indicates that Neu1 has recently emerged as a central target in sialidase-mediated regulation of diseases development, and plays a much more profound role in human diseases than previously expected. This paper summarized current progress of functional research on Neu1 in recent years, and the interacting mechanism between Neu1 and cell surface receptors.