Milk proteins are known for having a wide range of nutritional, functional and biological properties that make them important ingredients in functional or health promoting foods. These properties are partly attributed to bioactive peptides coded in the different milk proteins. Bioactive peptides are inactive within the protein sequence but may be released by the action of native proteolitic enzymes from milk, enzymes from lactic acid bacteria or from exogenous sources or may be produced during gastrointestinal digestion or processing of foods. Peptides derived from caseins and whey proteins were shown to present several bioactive properties such as opioid, antihypertensive, antimicrobial, immunodulatory, mineral carrier and antithrombotic. This overview presents a perspective of the importance of dairy proteins in the production of bioactive peptides and their biological activities, as well as the main analytical tecniques that have been used for the isolation and identification of these peptides.