GLP-1 peptide analogs for targeting pancreatic beta cells. Issue 8 (August 2021)

• Record Type: Journal Article
• Authors: Alavi, Seyed Ebrahim; Ebrahimi Shahmabadi, Hasan
• Is Part Of: Drug discovery today. Volume 26:Issue 8(2021)
• Page Start: 1936
• Page End: 1943
• Publication Date: 2021-08
• Subjects: Diabetes -- Drug delivery -- Glucagon-like peptide 1 -- Pancreatic beta cells -- Imaging; Drugs -- Design -- Periodicals; Drugs -- Research -- Periodicals; 615.1
• DOI: 10.1016/j.drudis.2021.03.032
• Languages: English
• ISSNs: 1359-6446

Abstract

Highlights: Targeting pancreatic beta cells is a promising approach to treat pancreatic beta-cell disorders. GLP-1R signaling is responsible for controlling glucose homeostasis. GLP-1 analogs are promising ligands for targeting GLP-1R. Exendin-4 analogs are metabolically stable GLP-1 analogs used for targeting GLP-1R. GLP-1 stability can be improved by sequence modification, conjugation to other compounds, and drug delivery systems. Abstract: Loss or dysfunction of the pancreatic beta cells or insulin receptors leads to diabetes mellitus (DM). This usually occurs over many years; therefore, the development of methods for the timely detection and clinical intervention are vital to prevent the development of this disease. Glucagon-like peptide-1 receptor (GLP-1R) is the receptor of GLP-1, an incretin hormone that causes insulin secretion in a glucose-dependent manner. GLP-1R is highly expressed on the surface of pancreatic beta cells, providing a potential target for bioimaging. In this review, we provide an overview of various strategies, such as the development of GLP-1R agonists (e.g., exendin-4), and GLP-1 sequence modifications for GLP-1R targeting for the diagnosis and treatment of pancreatic beta cell disorders. We also discuss the challenges of targeting pancreatic beta cells and strategies to address such challenges.