There has been heightened effort to discover bioactive peptides from food and uncover their human health benefits based on preclinical evaluation systems. Consequently, a myriad of bioactive peptides are continuously reported with emerging interest in elucidating structure–function and molecular mechanisms. However, there is limited clinical evidence to substantiate bioactivity and minimal emphasis on translation into functional peptide products for health uses. This paper highlights the prospects of bioinformatics and a proposed integrated approach for enhancing the production of existing and new bioactive peptides from sustainable food protein sources, followed by discussion of the major challenges that may impact prospective commercialization of food bioactive peptides for use in human health promotion.