Pharmacology, Physiology, and Mechanisms of Action of Dipeptidyl Peptidase-4 Inhibitors
University of Toronto · Lunenfeld-Tanenbaum Research Institute
Abstract
Dipeptidyl peptidase-4 (DPP4) is a widely expressed enzyme transducing actions through an anchored transmembrane molecule and a soluble circulating protein. Both membrane-associated and soluble DPP4 exert catalytic activity, cleaving proteins containing a position 2 alanine or proline. DPP4-mediated enzymatic cleavage alternatively inactivates peptides or generates new bioactive moieties that may exert competing or novel activities. The widespread use of selective DPP4 inhibitors for the treatment of type 2 diabetes has heightened interest in the molecular mechanisms through which DPP4 inhibitors exert their pleiotropic actions. Here we review the biology of DPP4 with a focus on: 1) identification of…
Citation impact
- FWCI
- 16.41
- Percentile
- 100%
- References
- 242
Authors
2Topics & keywords
- Dipeptidyl peptidase-4
- Dipeptidyl peptidase
- Transmembrane protein
- Enzyme
- Chemistry
- Small molecule
- Biochemistry
- Drug discovery
- Good health and well-being