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Dipeptidylpeptidase IV (DPPIV) is a multifunctional protein expressed on the surface of a variety of cells, including epithelial cells, endothelial cells, and lymphocytes. It shares identity with T cell activating antigen CD26 and adenosine deaminase (adenosine deaminase) binding protein, and it is released in plasma in a soluble state. Substrates of CD26/DPPIV include a variety of proline-containing polypeptides, such as growth factors, chemokines, neuropeptides, and vasoactive peptides. DPPIV is involved in immune regulation, signal transduction and apoptosis, and plays an important role in tumor development. Importantly, DPPIV is a therapeutic target for type II diabetes, as it acts as a serum protease that can cleave incretin hormones in the polypeptide glucagon family to regulate the stability of glucose in the body.