{"entity": "publication", "iuid": "396cd29578c849e19721dd9a6187ec37", "timestamp": "2026-08-11T08:29:14.739Z", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/396cd29578c849e19721dd9a6187ec37.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/396cd29578c849e19721dd9a6187ec37"}}, "title": "Pre-clinical evaluation of [(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4 for imaging of insulinoma.", "authors": [{"family": "Selvaraju", "given": "Ram Kumar", "initials": "RK"}, {"family": "Velikyan", "given": "Irina", "initials": "I"}, {"family": "Asplund", "given": "Veronika", "initials": "V"}, {"family": "Johansson", "given": "Lars", "initials": "L"}, {"family": "Wu", "given": "Zhanhong", "initials": "Z"}, {"family": "Todorov", "given": "Ivan", "initials": "I"}, {"family": "Shively", "given": "Jack", "initials": "J"}, {"family": "Kandeel", "given": "Fouad", "initials": "F"}, {"family": "Eriksson", "given": "Barbro", "initials": "B"}, {"family": "Korsgren", "given": "Olle", "initials": "O"}, {"family": "Eriksson", "given": "Olof", "initials": "O"}], "type": "journal article", "published": "2014-07-00", "journal": {"title": "Nucl. Med. Biol.", "issn": "1872-9614", "volume": "41", "issue": "6", "pages": "471-476", "issn-l": "0969-8051"}, "abstract": "Insulinoma is the most common form of pancreatic endocrine tumors responsible for hyperinsulinism in adults. These tumors overexpress glucagon like peptide-1 (GLP-1) receptor, and biologically stable GLP-1 analogs have therefore been proposed as potential imaging agents. Here, we evaluate the potential of a positron emission tomography (PET) tracer, [(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4, for imaging and quantification of GLP-1 receptors (GLP-1R) in insulinoma.\n\n[(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4 was evaluated for binding to GLP-1R by in vitro autoradiography binding studies in INS-1 tumor from xenografts. In vivo biodistribution was investigated in healthy control mice, INS-1 xenografted and PANC1 xenografted immunodeficient mice at two different doses of peptide: 2.5\u03bcg/kg (baseline) and 100\u03bcg/kg (block). In vivo imaging of [(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4 in xenografted mice was evaluated by small animal PET/CT using a direct comparison with the clinically established insulinoma marker [(11)C]5-hydroxy-tryptophan ([(11)C]5-HTP).\n\nGLP-1 receptor density could be quantified in INS-1 tumor biopsies. [(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4 showed significant uptake (p\u22640.05) in GLP1-R positive tissues such as INS-1 tumor, lungs and pancreas upon comparison between baseline and blocking studies. In vivo imaging showed concordant results with higher tumor-to-muscle ratio in INS-1 xenografted mice compared with [(11)C]5-HTP.\n\n[(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4 has high affinity and specificity for GLP-1R expressed on insulinoma in vitro and in vivo.", "doi": "10.1016/j.nucmedbio.2014.03.017", "pmid": "24857864", "labels": {"Olof Eriksson": null, "SciLifeLab Fellow": null}, "xrefs": [{"db": "pii", "key": "S0969-8051(14)00092-4"}], "notes": [], "created": "2020-10-06T14:02:33.197Z", "modified": "2022-11-07T11:35:51.698Z"}