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DPP-4 inhibitors in the treatment of type 2 diabetes.

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DPP-4 inhibitors

Document type :
Article dans une revue scientifique
DOI :
10.1016/j.bcp.2011.11.028
PMID :
22172989
Title :
DPP-4 inhibitors in the treatment of type 2 diabetes.
DPP-4 inhibitors
Author(s) :
Duez, Helene [Auteur] refId
Récepteurs nucléaires, maladies cardiovasculaires et diabète - U 1011 [RNMCD]
Cariou, Bertrand [Auteur]
Institut du thorax
Staels, Bart [Auteur correspondant]
Récepteurs nucléaires, maladies cardiovasculaires et diabète - U 1011 [RNMCD]
Journal title :
Biochemical Pharmacology
Pages :
823-32
Publisher :
Elsevier
Publication date :
2012-04-01
ISSN :
0006-2952
English keyword(s) :
dipeptidylpeptidase (DPP)-4 inhibitors
gliptins
glucagon-like peptide (GLP)-1
glycemic control
type 2 diabetes
HAL domain(s) :
Sciences du Vivant [q-bio]/Biochimie, Biologie Moléculaire
English abstract : [en]
Although being a primary objective in the management of type 2 diabetes, optimal glycaemic control is difficult to achieve and usually not maintained over time. Type 2 diabetes is a complex pathology, comprising altered ...
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Although being a primary objective in the management of type 2 diabetes, optimal glycaemic control is difficult to achieve and usually not maintained over time. Type 2 diabetes is a complex pathology, comprising altered insulin sensitivity and impaired insulin secretion. Recent advances in the understanding of the physiological functions of incretins and their degrading enzyme dipeptidyl-peptidase (DPP)-4 have led to the 'discovery' of a new class of oral anti-diabetic drugs. Several DPP-4 inhibitors (or gliptins) with different chemical structures are now available. These agents inhibit the degradation of the incretins glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) and hence potentiate glucose-dependent insulin secretion. DPP-4 inhibitors inhibit DPP-4 activity by almost 100% in vitro, maintaining a ≥ 80% inhibition throughout the treatment period in vivo, thus prolonging GLP-1 half-life, and significantly reducing HbA1c generally by -0.7 to 0.8% as well as fasting and post-prandial glycaemia. They are well-tolerated with no weight gain and few adverse effects, and, of particular interest, no increase in hypoglycaemic episodes. Although different by their chemical structure and pharmacokinetic properties, the DPP4 inhibitors currently available have proven similar glucose lowering efficacy.Show less >
Language :
Anglais
Peer reviewed article :
Oui
Audience :
Internationale
Popular science :
Non
Collections :
  • Récepteurs nucléaires, Maladies Cardiovasculaires et Diabète (EGID) - U1011
Source :
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