GLP-1 peptide analogs for targeting pancreatic beta cells

Related Experiment Video

Updated: Nov 9, 2025

Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres
09:31

Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres

Published on: November 5, 2016

7.5K

Seyed Ebrahim Alavi1, Hasan Ebrahimi Shahmabadi1

  • 1Department of Microbiology, School of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan, Iran.

Drug Discovery Today
|April 11, 2021
PubMed

Insights

Targeting the glucagon-like peptide-1 receptor (GLP-1R) on pancreatic beta cells offers a promising strategy for early diabetes mellitus detection and treatment. This review explores GLP-1R targeting methods for improved diagnosis and intervention.

Area of Science:

  • Endocrinology
  • Molecular Imaging
  • Pharmacology

Background:

  • Diabetes mellitus (DM) results from pancreatic beta cell loss or dysfunction, necessitating early detection and intervention.
  • Glucagon-like peptide-1 receptor (GLP-1R), highly expressed on pancreatic beta cells, is a potential target for bioimaging and therapy.
  • GLP-1R is activated by the incretin hormone glucagon-like peptide-1 (GLP-1), which stimulates glucose-dependent insulin secretion.

Purpose of the Study:

  • To review strategies for targeting the GLP-1 receptor (GLP-1R) on pancreatic beta cells.
  • To explore the diagnostic and therapeutic potential of GLP-1R targeting for pancreatic beta cell disorders.
  • To discuss challenges and solutions in targeting pancreatic beta cells.

Main Methods:

  • Review of literature on GLP-1R agonists and modified GLP-1 sequences for targeting.
  • Analysis of strategies for bioimaging and therapeutic intervention via GLP-1R.
  • Discussion of challenges associated with pancreatic beta cell targeting.

Main Results:

  • GLP-1R agonists (e.g., exendin-4) and modified GLP-1 sequences show potential for GLP-1R targeting.
  • GLP-1R offers a viable target for the diagnosis and treatment of pancreatic beta cell disorders.
  • Various strategies exist for overcoming challenges in targeting pancreatic beta cells.

Conclusions:

  • Targeting GLP-1R on pancreatic beta cells is a promising avenue for managing diabetes mellitus.
  • Further development of GLP-1R targeting agents is crucial for clinical application.
  • Addressing targeting challenges will enhance the efficacy of pancreatic beta cell therapies.
Keywords:
DiabetesDrug deliveryGlucagon-like peptide 1ImagingPancreatic beta cells

More Related Videos

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine07:00

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

Published on: February 26, 2019

9.8K
A High-content In Vitro Pancreatic Islet β-cell Replication Discovery Platform09:35

A High-content In Vitro Pancreatic Islet β-cell Replication Discovery Platform

Published on: July 16, 2016

11.4K

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...
538
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...
327
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...
372
Insulin: Biosynthesis, Chemistry, and Preparation01:25

Insulin: Biosynthesis, Chemistry, and Preparation

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...
781
Glucose Homeostasis: Pancreatic Islets and Insulin Secretion01:27

Glucose Homeostasis: Pancreatic Islets and Insulin Secretion

The pancreatic islets comprising only 1%-2% of the volume are highly vascularized and innervated mini-organs. They contain five endocrine cell types, including β cells that secrete insulin, which is synthesized as a single polypeptide chain, preproinsulin, processed to proinsulin, and finally to insulin and C-peptide. This process is complex and regulated, involving the Golgi complex, the endoplasmic reticulum, and the secretory granules of the β cell.
Insulin and C-peptide are...
1.7K
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...
363