Related Experiment Video
Updated: Sep 19, 2025
07:00
Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
Published on: February 26, 2019
9.6K
GLP-1R in diabetes mellitus: from basic discovery to therapeutics development
Shujun Li1, Nanqu Huang2,3, Mei Wang4
1Key Laboratory of Basic Pharmacology and Joint International Research Laboratory of Ethnomedicine of Ministry of Education, Zunyi Medical University, Zunyi, Guizhou, China.
Frontiers in Pharmacology
|June 16, 2025
Summary
Glucagon-like peptide-1 receptor (GLP-1R) is a key target for treating diabetes mellitus. GLP-1R agonists show promise in managing blood sugar and related complications.
Area of Science:
- Endocrinology
- Pharmacology
Background:
- Diabetes mellitus (DM) is a global health challenge characterized by hyperglycemia.
- Glucagon-like peptide-1 receptor (GLP-1R) is a G protein-coupled receptor crucial for glucose homeostasis.
- GLP-1R is expressed in various tissues, including pancreatic islets, CNS, and GI tract.
Purpose of the Study:
- To review the structural and functional characteristics of GLP-1R.
- To explore the role of GLP-1R in glucose homeostasis and its therapeutic applications in diabetes.
- To summarize the clinical progress of GLP-1R agonists.
Main Methods:
- Literature review of GLP-1R structure, function, and clinical applications.
- Analysis of GLP-1R mechanisms in pancreatic islets, CNS, and GI tract.
- Evaluation of clinical data on GLP-1R agonists' efficacy and safety.
Main Results:
- GLP-1R activation enhances insulin secretion and inhibits glucagon secretion.
- GLP-1R plays a role in β-cell protection, delayed gastric emptying, and satiety.
- GLP-1R agonists demonstrate clinical efficacy and safety in diabetes treatment.
Conclusions:
- GLP-1R is a significant therapeutic target for diabetes mellitus.
- GLP-1R agonists offer a promising approach for managing diabetes and its complications.
- Further research into GLP-1R pathways may yield novel treatment strategies.
Related Concept Videos
01:24Glucagon-like Receptor Agonists
438
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...
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...
438
01:06Oral Hypoglycemic Agents: Glinides
274
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...
274
01:23Dipeptidyl Peptidase 4 Inhibitors
271
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...
271
01:25Insulin: Biosynthesis, Chemistry, and Preparation
570
The endoplasmic reticulum (ER) of pancreatic β-cells synthesizes preproinsulin, which consists of a signal peptide, A and B chains, and a C-peptide. Preproinsulin is then cleaved and folded into proinsulin, which translocates to the Golgi apparatus for sorting and packaging into secretory granules. In these granules, enzymatic clipping generates insulin and C-peptide.
Damage or functional impairment of β-cells inhibits insulin production, leading to diabetes. Diabetes treatment...
Damage or functional impairment of β-cells inhibits insulin production, leading to diabetes. Diabetes treatment...
570
01:28Insulin: The Receptor and Signaling Pathways
1.5K
Insulin action is mediated through a receptor tyrosine kinase, akin to the IGF-1 receptor. The number of receptors per cell varies significantly, from 40 on erythrocytes to 300,000 on adipocytes and hepatocytes. The insulin receptor consists of linked α/β subunit dimers, forming a heterotetramer glycoprotein with two extracellular α subunits and two β subunits spanning the membrane. The α subunits inhibit the inherent tyrosine kinase activity of the β subunits, but...
1.5K
01:26Oral Hypoglycemic Agents: Biguanides and Glitazones
310
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...
310