Berries contain powerful antioxidants, potential allergens, and other bioactive compounds. Genetic and environmental factors affect production and storage of such compounds. For this reason breeding and biotechnological approaches are currently used to control or to increase the content of specific health-related compounds in fruits. This work reviews the main bioactive compounds determining the nutritional quality of berries, the major factors affecting their content and activity, and the genetic options currently available to achieve new genotypes able to provide, under controlled cultivation conditions, berries with the proper balance of bioactive compounds for improving consumer health.