Dipeptidyl peptidase IV: An attractive target for the development of effective diagnostic and therapeutic strategies

Abstract

DPP IV is a peptidase with a catalytic activity and the ability to bind extracellular matrix proteins. It participates in the metabolism of glucose, gastrointestinal motility, the regulation of appetite and affects the function of the immune system. It is also involved in the formation of pain and inflammation. The variety of activities due to extensive expression in endothelial and epithelial cells makes the enzyme a promising tool for diagnostic and prognostic applications. The natural DPP IV peptide inhibitors and substrates have inspired the search for new, therapeutically important compounds that selectively inhibit the enzyme activity. A number of changes to the structure of the parent molecules have been required to improve their pharmacokinetic and pharmacodynamic profile to achieve therapeutic efficacy. The several synthetic scaffold mimetics, known as gliptins, are now in clinical use in the treatment of diabetes mellitus type 2. Recent studies indicate that gliptin inhibitors may be of therapeutic interest or inspiration for the development of new drugs for other diseases such as cancer, inflammatory, degenerative diseases, metabolic and neurological disorders or dysfunctions of the immune system.