Peptides are functional active fragments of proteins which can provide nutrients needed for human growth and development, and they also have unique physiological activity characteristics relative to proteins.  Bioactive peptides contain a great deal of development potential.  More specifically, food-derived bioactive peptides have the advantages of a wide variety of sources, unique structures, high efficiency and safety, so they have broad development prospects.  This review provides an overview of the current advances regarding the preparation, functional characteristics, and structure–activity relationships of food-derived bioactive peptides.  Moreover, the prospects for the future development and application of food-derived bioactive peptides are discussed.  This review may provide a better understanding of food-derived bioactive peptides, and some constructive inspirations for further research and applications in the food industry.