GLPwatch
Multivalent γ-PGA-Exendin-4 Conjugates to Target Pancreatic β-Cells.
Chembiochem · 2022
Last updated 2026-05-28Researchers combined the diabetes drug exendin-4 with a polymer called γ-PGA to create a more stable version that targets pancreatic β-cells. In lab tests, the new compound with an average of 120 exendin-4 molecules per polymer chain showed twice the binding strength to the GLP-1 receptor compared to the original drug.
AI summary of the abstract below.
| Journal | Chembiochem, 2022 |
|---|---|
| Citations | 2 |
| Relative citation ratio | 0.25 |
| NIH percentile | 16 |
| Molecules | — |
| Conditions studied | Type 2 Diabetes |
Abstract
Targeting of glucagon-like peptide 1 receptor (GLP-1R), expressed on the surface of pancreatic β-cells, is of great interest for the development of advanced therapies for diabetes and diagnostics for insulinoma. We report the conjugation of exendin-4 (Ex-4), an approved drug to treat type 2 diabetes, to poly-γ-glutamic acid (γ-PGA) to obtain more stable and effective GLP-1R ligands. Exendin-4 modified at Lysine-27 with PEG4-maleimide was conjugated to γ-PGA functionalized with furan, in different molar ratios, exploiting a chemoselective Diels-Alder cycloaddition. The γ-PGA presenting the highest number of conjugated Ex-4 molecules (average 120 per polymeric chain) showed a double affinity towards GLP-1R with respect to exendin per se, paving the way to improved therapeutic and diagnostic applications.
Verbatim abstract via PubMed 35762648 ↗