Do we know the true mechanism of action of the DPP-4 inhibitors?
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Do we know the true mechanism of action of the DPP-4 inhibitors? / Andersen, Emilie S.; Deacon, Carolyn F.; Holst, Jens Juul.
In: Diabetes, Obesity and Metabolism, Vol. 20, No. 1, 2018, p. 34-41.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Do we know the true mechanism of action of the DPP-4 inhibitors?
AU - Andersen, Emilie S.
AU - Deacon, Carolyn F.
AU - Holst, Jens Juul
PY - 2018
Y1 - 2018
N2 - The prevalence of type 2 diabetes is increasing, which is alarming because of its serious complications. Anti-diabetic treatment aims to control glucose homeostasis as tightly as possible in order to reduce these complications. Dipeptidyl peptidase-4 (DPP-4) inhibitors are a recent addition to the anti-diabetic treatment modalities, and have become widely accepted because of their good efficacy, their benign side-effect profile and their low hypoglycaemia risk. The actions of DPP-4 inhibitors are not direct, but rather are mediated indirectly through preservation of the substrates they protect from degradation. The two incretin hormones, glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide, are known substrates, but other incretin-independent mechanisms may also be involved. It seems likely therefore that the mechanisms of action of DPP-4 inhibitors are more complex than originally thought, and may involve several substrates and encompass local paracrine, systemic endocrine and neural pathways, which are discussed here.
AB - The prevalence of type 2 diabetes is increasing, which is alarming because of its serious complications. Anti-diabetic treatment aims to control glucose homeostasis as tightly as possible in order to reduce these complications. Dipeptidyl peptidase-4 (DPP-4) inhibitors are a recent addition to the anti-diabetic treatment modalities, and have become widely accepted because of their good efficacy, their benign side-effect profile and their low hypoglycaemia risk. The actions of DPP-4 inhibitors are not direct, but rather are mediated indirectly through preservation of the substrates they protect from degradation. The two incretin hormones, glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide, are known substrates, but other incretin-independent mechanisms may also be involved. It seems likely therefore that the mechanisms of action of DPP-4 inhibitors are more complex than originally thought, and may involve several substrates and encompass local paracrine, systemic endocrine and neural pathways, which are discussed here.
KW - dipeptidyl peptidase-4 inhibitors
KW - incretin therapy
KW - type 2 diabetes
U2 - 10.1111/dom.13018
DO - 10.1111/dom.13018
M3 - Journal article
C2 - 28544214
VL - 20
SP - 34
EP - 41
JO - Diabetes, Obesity and Metabolism
JF - Diabetes, Obesity and Metabolism
SN - 1462-8902
IS - 1
ER -
ID: 195511468