Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?

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State: Public
Version: author
Serval ID
serval:BIB_4435273D9544
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Institution
Title
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?
Journal
Journal of Medicinal Chemistry
Author(s)
Juillerat-Jeanneret L.
ISSN
1520-4804 (Electronic)
ISSN-L
0022-2623
Publication state
Published
Issued date
2014
Peer-reviewed
Oui
Volume
57
Number
6
Pages
2197-2212
Language
english
Notes
Publication types: Journal Article ; Review : PDF : perspective
Abstract
The proline-specific dipeptidyl aminopeptidase IV (DPP IV, DPP-4, CD26), widely expressed in mammalians, releases X-Pro/Ala dipeptides from the N-terminus of peptides. DPP IV is responsible of the degradation of the incretin peptide hormones regulating blood glucose levels. Several families of DPP IV inhibitors have been synthesized and evaluated. Their positive effects on the degradation of the incretins and the control of blood glucose levels have been demonstrated in biological models and in clinical trials. Presently, several DPP IV inhibitors, the "gliptins", are approved for type 2 diabetes or are under clinical evaluation. However, the gliptins may also be of therapeutic interest for other diseases beyond the inhibition of incretin degradation. In this Perspective, the biological functions and potential substrates of DPP IV enzymes are reviewed and the characteristics of the DPP IV inhibitors are discussed in view of type 2 diabetes and further therapeutic interest.
Keywords
Animals, Diabetes Mellitus, Type 2/drug therapy, Dipeptidyl Peptidase 4/chemistry, Dipeptidyl Peptidase 4/metabolism, Dipeptidyl-Peptidase IV Inhibitors/chemistry, Dipeptidyl-Peptidase IV Inhibitors/pharmacology, Humans, Structure-Activity Relationship
Pubmed
Web of science
Create date
11/12/2013 10:03
Last modification date
20/08/2019 14:48
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