Dipeptidyl-peptidase 4 Inhibition: Linking Metabolic Control to Cardiovascular Protection

Author(s): Angelo Avogaro, Saula de Kreutzenberg, Gianpaolo Fadini

Journal Name: Current Pharmaceutical Design

Volume 20 , Issue 14 , 2014

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Dipeptidyl peptidases 4 (DPP4) inhibitors are a new class of oral anti-hyperglycemic drugs for the treatment of type 2 diabetes (T2DM). They are also called “incretins” because they act by inhibiting the degradation of endogenous incretin hormones, in particular GLP-1, that mediates their main metabolic effects. DPP4 is an ubiquitous protease that regulates not only glucose and lipid metabolism, but also exhibits several systemic effects at different site levels. DPP4 inhibition improves endothelial function, reduces the pro-oxidative and the pro-inflammatory state, and exerts renal effects. These actions are mediated by different DPP4 ligands, such as cytokines, growth factors, neuotransmitters etc. Clinical and experimental studies have demonstrated that DPP4 inhibitors are efficient in protecting cardiac, renal and vascular systems, through antiatherosclerotic and vasculoprotective mechanisms. For these reasons DDP4 inhibitors are thought to be “cardiovascular protective” as well as anti-diabetic drugs. Clinical trials aimed to demonstrate the efficacy of DPP4 inhibitors in reducing cardiovascular events, independent of their anti-hyperglycemic action, are ongoing. These trials will also give necessary information on their safety.

Keywords: Dipeptidyl peptidases, diabetes mellitus, cardiovascular system, incretins.

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Article Details

Year: 2014
Page: [2387 - 2394]
Pages: 8
DOI: 10.2174/13816128113199990474

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