Sponsored Content by ACROBiosystemsReviewed by Aimee MolineuxSep 10 2024 In 2023, the global market for anti-obesity drugs reached US $ 6 billion. Goldman Sachs forecasts a more than 16-fold increase by 2030, reaching a total of $100 billion.Recently, the glucago*-like peptide-1 receptor has become a primary target in diabetes and obesity treatment because of its role in controlling blood sugar and weight.
If no ligand is present, weak interactions between the ECD and TMD prevent receptor activation by blocking ligand binding, acting as a negative regulatory mechanism.GLP-1R’s biological functions GLP-1R is extensively distributed throughout the body, including in the pancreatic beta cells, the stomach, the intestines, the brain, and the heart. It interacts with GLP-1 to control insulin secretion and blood sugar levels.
GLP-1R's high affinity for peptide ligands makes peptide-based therapeutics the main form of GLP-1R-targeted therapies. However, the native GLP-1 molecule is rapidly degraded by dipeptidyl peptidase-4 and glomerular filtration and requires modifications to extend its half-life. Glutazumab Glutazumab is a novel antibody-drug that targets GLP-1R directly. It was created for the treatment of obesity and type 2 diabetes and features a fusion of a 23-amino-acid peptide linker and a DPP-4-resistant GLP-1 fragment attached to the light chain of a humanized GLP-1R antibody.
It has three domains: a mutated GLP-1 fragment with enhanced DPP-4 resistance, a humanized human serum albumin nanobody that binds HSA to extend half-life by preventing rapid clearance, and a humanized GLP-1R nanobody that activates the GLP-1R signaling pathway upon dissociation from HSA.