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Dipeptidyl Peptidase 4 Inhibitors01:23

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
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The therapy for diabetes aims to alleviate hyperglycemia-related symptoms, prevent acute metabolic decompensation, and reduce chronic end-organ complications. Glycemic control is evaluated through short-term (self-monitoring, continuous glucose monitoring) and long-term (A1c, fructosamine) metrics, enabling near real-time tracking of blood glucose levels and reflecting glycemic control over specific time frames.
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GLP-1 based therapeutics: simultaneously combating T2DM and obesity.

Kristy M Heppner1, Diego Perez-Tilve2

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Frontiers in Neuroscience
|April 9, 2015
PubMed
Summary

Glucagon-like peptide-1 (GLP-1) receptor agonists improve blood sugar and promote weight loss in type II diabetes patients. This review covers GLP-1R

Keywords:
CNSGLP-1diabetesinsulinobesity

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Area of Science:

  • Endocrinology
  • Metabolic Diseases
  • Pharmacology

Background:

  • Glucagon-like peptide-1 (GLP-1) is an incretin hormone that enhances insulin secretion and lowers blood glucose.
  • GLP-1 also acts in the brain via the GLP-1 receptor (GLP-1R) to suppress appetite.
  • GLP-1R agonists are used to treat type II diabetes (T2DM).

Purpose of the Study:

  • To review the mechanisms of GLP-1R action on energy and glucose metabolism.
  • To evaluate the effectiveness of GLP-1R agonists for weight loss in T2DM patients.
  • To discuss GLP-1R combination therapies.

Main Methods:

  • Literature review of studies on GLP-1R signaling and its metabolic effects.
  • Analysis of clinical trial data on GLP-1R agonists for T2DM treatment.
  • Synthesis of information on combination therapies involving GLP-1R agonists.

Main Results:

  • GLP-1R signaling improves glycemic control and promotes significant weight loss in T2DM patients.
  • Unlike many other T2DM medications, GLP-1R agonists are associated with weight reduction.
  • Combination therapies may offer enhanced benefits for T2DM management.

Conclusions:

  • GLP-1R agonists represent a valuable therapeutic option for T2DM, offering dual benefits of glycemic control and weight loss.
  • The central appetite-suppressing effects of GLP-1R are crucial for its weight-reducing efficacy.
  • Further research into GLP-1R combination therapies could optimize T2DM treatment strategies.