Enzymatic synthesis of peptides has attracted a great deal of attention in recent years. The proteases from bacterial, fungal, plant, and animal sources have been successfully applied to the synthesis of several small peptides, mainly dipeptides and tripeptides. Peptide bonds can be synthesized using proteases in either a thermodynamically controlled or a kinetically controlled manner. The development of new methods suitable for the large-scale production of biologically active peptides has been actively pursued over the last decade due to their bioactive nature as well as better understanding of their biological functions and properties. The aim of this study was to review the basic techniques of peptide synthesis and some advancement in biotechnological methods for their production.