First-in-class positron emission tomography tracer for the glucagon receptor.

ABSTRACT: The glucagon receptor (GCGR) is emerging as an important target in anti-diabetic therapy, especially as part of the pharmacology of dual glucagon-like peptide-1/glucagon (GLP-1/GCG) receptor agonists. However, currently, there are no suitable biomarkers that reliably demonstrate GCG receptor target engagement.

Methods

Two potent GCG receptor peptide agonists, S01-GCG and S02-GCG, were labeled with positron emission tomography (PET) radionuclide gallium-68. The GCG receptor binding affinity and specificity of the resulting radiopharmaceuticals [⁶⁸Ga]Ga-DO3A-S01-GCG and [⁶⁸Ga]Ga-DO3A-S02-GCG were evaluated in HEK-293 cells overexpressing the human GCG receptor and on frozen hepatic sections from human, non-human primate, and rat. In in vivo biodistribution, bindi

SUBMITTER: Velikyan I 

PROVIDER: S-EPMC6377692 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature