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Related Concept Videos

Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
250
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

109
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...
109
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

117
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...
117
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

106
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.
Acarbose and miglitol are...
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Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
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Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

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Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood...
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Related Experiment Video

Updated: May 9, 2025

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
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GLP-1R agonists: recent advances, current gaps, and future challenges.

Anukriti Saran1, Riya Raisinghani2, Sarvesh Paliwal3

  • 1Department of Bioscience and Biotechnology, Banasthali Vidyapith, Banasthali, Rajasthan, 304022, India. anukritisaransingh@gmail.com.

Molecular Diversity
|April 29, 2025
PubMed
Summary

Glucagon-like peptide-1 receptor agonists (GLP-1RAs) effectively manage type 2 diabetes, kidney disease, and obesity. This review covers available, investigational, and withdrawn GLP-1RAs, their side effects, and future drug discovery.

Keywords:
Glucagon-like peptide-1Glucagon-like peptide-1 receptorGlucagon-like peptide-1 receptor agonistsSemaglutide

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Area of Science:

  • Pharmacology
  • Endocrinology
  • Metabolic Diseases

Background:

  • Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are crucial in managing glucose metabolism disorders.
  • GLP-1RAs demonstrate efficacy in type 2 diabetes mellitus (T2DM), chronic kidney disease (CKD), cardiovascular conditions, and non-alcoholic fatty liver disease (NAFLD).
  • Obesity management is another key indication for GLP-1RA therapy.

Purpose of the Study:

  • To review available, withdrawn, and investigational GLP-1 receptor agonists.
  • To explore the common side effects and safety profiles of GLP-1RAs.
  • To highlight recent advances and challenges in GLP-1RA drug discovery.

Main Methods:

  • Literature review of GLP-1 receptor agonists.
  • Analysis of drug classes including liraglutide, exenatide, and semaglutide.
  • Examination of safety profiles and efficacy data.

Main Results:

  • Semaglutide is noted as a recent GLP-1RA available in oral and subcutaneous formulations.
  • The review categorizes GLP-1RAs into available, withdrawn, and investigational.
  • Common side effects and safety data for short-acting and long-acting GLP-1RAs are discussed.

Conclusions:

  • GLP-1RAs represent a significant therapeutic class for metabolic and related diseases.
  • Understanding the safety and efficacy profiles of various GLP-1RAs is essential for clinical practice.
  • Continued research in GLP-1RA drug discovery is vital for addressing unmet medical needs.