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Related Concept Videos

Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

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 the...
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

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 manages...
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

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

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

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 typically...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

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 glucose levels...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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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Related Experiment Video

Updated: May 30, 2026

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
07:00

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine

Published on: February 26, 2019

GLP-1 receptor agonists today.

Michel Marre1, Alfred Penfornis

  • 1Department of Endocrinology, Diabetology and Nutrition, Bichat Hospital, Assistance Publique des Hôpitaux de Paris, 46 rue Henri Huchard, 75877 Paris Cedex 18, France. michel.marre@bch.aphp.fr

Diabetes Research and Clinical Practice
|July 20, 2011
PubMed
Summary
This summary is machine-generated.

Glucagon-like peptide-1 (GLP-1) receptor agonists offer new hope for managing type 2 diabetes, addressing unmet needs in glycaemic control and reducing complication risks. This review explores their current and future roles in diabetes therapy.

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Mixed Primary Cultures of Murine Small Intestine Intended for the Study of Gut Hormone Secretion and Live Cell Imaging of Enteroendocrine Cells
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Mixed Primary Cultures of Murine Small Intestine Intended for the Study of Gut Hormone Secretion and Live Cell Imaging of Enteroendocrine Cells

Published on: April 20, 2017

Measuring Relative Insulin Secretion using a Co-Secreted Luciferase Surrogate
05:58

Measuring Relative Insulin Secretion using a Co-Secreted Luciferase Surrogate

Published on: June 25, 2019

Related Experiment Videos

Last Updated: May 30, 2026

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
07:00

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine

Published on: February 26, 2019

Mixed Primary Cultures of Murine Small Intestine Intended for the Study of Gut Hormone Secretion and Live Cell Imaging of Enteroendocrine Cells
09:16

Mixed Primary Cultures of Murine Small Intestine Intended for the Study of Gut Hormone Secretion and Live Cell Imaging of Enteroendocrine Cells

Published on: April 20, 2017

Measuring Relative Insulin Secretion using a Co-Secreted Luciferase Surrogate
05:58

Measuring Relative Insulin Secretion using a Co-Secreted Luciferase Surrogate

Published on: June 25, 2019

Area of Science:

  • Endocrinology and Metabolism
  • Pharmacology
  • Diabetes Research

Background:

  • Type 2 diabetes mellitus (T2DM) affects millions globally, with significant unmet needs in current treatment paradigms.
  • Traditional T2DM therapies often result in suboptimal glycaemic control and elevated risks of diabetes-related complications.
  • Emerging therapeutic classes, such as GLP-1 receptor agonists, show promise in addressing these limitations.

Purpose of the Study:

  • To review current clinical guidelines and recent findings on approved glucagon-like peptide-1 (GLP-1) receptor agonists.
  • To explore novel GLP-1 receptor agonists currently under development.
  • To examine the physiological rationale for early GLP-1 receptor agonist use, their role as insulin alternatives, combination therapy potential, and cost-effectiveness.

Main Methods:

  • Comprehensive literature review of recent findings and clinical guidelines.
  • Analysis of physiological mechanisms underlying GLP-1 receptor agonist action.
  • Evaluation of evidence regarding therapeutic positioning, including early use, insulin substitution, and combination strategies.

Main Results:

  • Approved GLP-1 receptor agonists demonstrate efficacy in improving glycaemic control and addressing unmet needs in T2DM management.
  • New GLP-1 receptor agonists in development offer potential for enhanced efficacy and expanded therapeutic options.
  • Evidence supports the use of GLP-1 receptor agonists as an alternative to or in combination with insulin therapy, with considerations for cost-effectiveness.

Conclusions:

  • GLP-1 receptor agonists represent a significant advancement in T2DM therapeutics, addressing key limitations of traditional treatments.
  • The review highlights the evolving landscape of GLP-1 receptor agonists, from current approved agents to promising future developments.
  • Strategic implementation, including early use and combination therapy, alongside cost-effectiveness analyses, will be crucial for optimizing patient outcomes in T2DM.