GLP-1 peptide analogs for targeting pancreatic beta cells

Drug Discov Today. 2021 Aug;26(8):1936-1943. doi: 10.1016/j.drudis.2021.03.032. Epub 2021 Apr 9.

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.

Keywords: Diabetes; Drug delivery; Glucagon-like peptide 1; Imaging; Pancreatic beta cells.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus / drug therapy
  • Diabetes Mellitus / prevention & control
  • Drug Development
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide-1 Receptor Agonists*
  • Glucose / metabolism
  • Humans
  • Hypoglycemic Agents / pharmacology*
  • Insulin / metabolism
  • Insulin-Secreting Cells / pathology

Substances

  • Hypoglycemic Agents
  • Insulin
  • Glucagon-Like Peptide 1
  • Glucose
  • Glucagon-Like Peptide-1 Receptor Agonists