Fig. 2
From: DPP-4 inhibitors and GLP-1RAs: cardiovascular safety and benefits
Incretin axis and incretin-based therapies: GLP-1 is produced by the enteroendocrine L-cells in response to meal ingestion. The active form of GLP-1 is rapidly inactivated by DPP-4. GLP-1 acts on pancreas, liver, gastrointestinal tract, adipose tissue, cardiovascular system, and brain to exert a variety of functions. The rapid inactivation by DPP-4 in vivo limits the application of GLP-1 in clinic. The development of DPP-4 resistant analogues (GLP-1RAs) and DPP-4i overcame the instability shortcoming of GLP-1 and became an important class of glycemic lowering drugs that are safe or beneficial to cardiovascular disease. GLP-1RAs reduce multiple cardiovascular risks such as hypertension, hyperglycemia, dyslipidemia, overweight, and insulin resistance via various mechanisms. DPP-4 dipeptidyl peptidase-4, DPP-4i DPP-4 inhibitors, GLP-1 glucagon-like peptide-1, ApoB48 apolipoprotein B48, VLDL very low-density lipoprotein, LDL low-density lipoprotein