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Dipeptidyl peptidase 4 (DPP-4) is an enzyme that plays a crucial role in the regulation of glucose metabolism. It is part of the DPP-4 inhibitor class of drugs and is primarily involved in the breakdown of incretin hormones, including glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). By inhibiting DPP-4, these drugs increase the levels of GLP-1 and GIP, resulting in improved glycemic control in individuals with type 2 diabetes.
DPP-4 inhibitors are widely used in the management of type 2 diabetes mellitus. They are often prescribed as an add-on therapy to diet and exercise or as part of a combination therapy with other antidiabetic medications, such as metformin. DPP-4 inhibitors help lower blood glucose levels by enhancing insulin secretion and reducing glucagon release, thereby improving overall glycemic control.
DPP-4 is found in various tissues and organs throughout the body, including the gastrointestinal tract, liver, kidneys, and immune cells. However, it is primarily expressed on the surface of immune cells, such as T cells, B cells, and natural killer cells. In the gastrointestinal tract, DPP-4 is present on the brush border of intestinal epithelial cells, where it regulates the stability and levels of incretin hormones.
- Improved glycemic control: DPP-4 inhibitors help lower blood glucose levels in individuals with type 2 diabetes by increasing the levels of GLP-1 and GIP, which enhance insulin secretion and reduce glucagon release. This leads to improved glycemic control and a reduction in HbA1c levels.
- Weight management: DPP-4 inhibitors have been shown to be weight-neutral or even associated with modest weight loss compared to other antidiabetic medications. This can be beneficial for individuals with type 2 diabetes who are overweight or obese.
- Cardiovascular protection: Several studies have suggested that DPP-4 inhibitors may have cardiovascular benefits, including a reduction in the risk of major adverse cardiovascular events. These drugs have shown favorable effects on markers of inflammation, endothelial function, and oxidative stress, which may contribute to their cardioprotective effects.
- Renal function preservation: DPP-4 inhibitors have been shown to preserve renal function and reduce albuminuria in individuals with type 2 diabetes. This can help slow the progression of diabetic nephropathy and protect against kidney damage.
- Safety profile: DPP-4 inhibitors have a favorable safety profile, with a low risk of hypoglycemia compared to some other antidiabetic medications. They are generally well-tolerated, with minimal side effects.
- DPP-4 inhibitors were first approved for use in the management of type 2 diabetes in 2006.
- The incretin hormones GLP-1 and GIP, which are regulated by DPP-4, play important roles in glucose homeostasis and appetite control.
- DPP-4 inhibitors are available in oral tablet form and are usually taken once daily.
- The use of DPP-4 inhibitors has been associated with a lower risk of hypoglycemia compared to insulin and sulfonylureas.
- Tripeptide
- Tetrapeptide
- Pentapeptide
