DPP-4 Inhibition: A Means to Achieve
Enhancement of Intact Incretins

 

  • After release, GLP-1 (7-36) and GIP (1-42) are rapidly metabolized by the enzyme DPP-44,7, which is located in various tissues, on the capillary surfaces, and in soluble form in the circulation.15
  • DPP-4 cleaves off the first two amino acids from the intact peptides, producing two truncated peptides, GLP-1(9-36) and GIP(3-42),5,7,16 that are mainly eliminated through the kidneys.8,17
  • These truncated peptides do not activate the respective GLP-1 or GIP receptors17 and do not affect insulin release or glucose control.15,18

DPP-4 inhibition has been shown to prevent the rapid degradation of GLP-1 and GIP to their truncated forms, therefore prolonging the survival of GLP-1 (7-36) and GIP (1-42) and their beneficial actions in glucose regulation.7,19,20

MECHANISM OF ACTION
Mechanism of Action Video
 
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