Parkinson"s disease (PD) is the second most common neurodegenerative disease. The pathological aggregation of α-synuclein (α-syn) is a biomarker of PD, which is closely related to the occurrence and development of PD. Finding an inhibitor that can inhibit the formation of pathological aggregates such as α-syn Oligomer and α-syn fibrils at the early stage of the disease is of great significance for the treatment of PD. In recent years, significant progress has been made in the research of aggregation inhibitors targeting α-syn. This review summarizes the structure, physiological function, pathological mechanism and aggregation inhibitors of α-synuclein, aiming to provide a reference for the further research and development of α-syn aggregation inhibitors.