First-in-class positron emission tomography tracer for the glucagon receptor.
Dual agonist
GCG
GLP-1 receptor
Glucagon
Type 2 diabetes
Journal
EJNMMI research
ISSN: 2191-219X
Titre abrégé: EJNMMI Res
Pays: Germany
ID NLM: 101560946
Informations de publication
Date de publication:
15 Feb 2019
15 Feb 2019
Historique:
received:
12
10
2018
accepted:
25
01
2019
entrez:
17
2
2019
pubmed:
17
2
2019
medline:
17
2
2019
Statut:
epublish
Résumé
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. 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 [ [ [
Identifiants
pubmed: 30771019
doi: 10.1186/s13550-019-0482-0
pii: 10.1186/s13550-019-0482-0
pmc: PMC6377692
doi:
Types de publication
Journal Article
Langues
eng
Pagination
17Subventions
Organisme : Sanofi-Aventis
ID : N/A
Références
Bioconjug Chem. 2004 May-Jun;15(3):554-60
pubmed: 15149183
Nat Chem Biol. 2009 Oct;5(10):749-57
pubmed: 19597507
Diabetes. 2009 Oct;58(10):2258-66
pubmed: 19602537
Eur J Nucl Med Mol Imaging. 2010 Jul;37(7):1345-55
pubmed: 20111963
J Nucl Med. 2013 Aug;54(8):1458-63
pubmed: 23761918
Diabetologia. 2014 May;57(5):950-9
pubmed: 24488022
J Clin Endocrinol Metab. 2014 May;99(5):1519-24
pubmed: 24512490
Eur J Nucl Med Mol Imaging. 2014 Sep;41(9):1800-10
pubmed: 24643781
Am J Nucl Med Mol Imaging. 2015 Feb 15;5(3):259-69
pubmed: 26069859
J Med Chem. 2017 May 25;60(10):4293-4303
pubmed: 28448133
Diabetologia. 2017 Oct;60(10):1851-1861
pubmed: 28733905
Acta Diabetol. 2017 Nov;54(11):1039-1045
pubmed: 28891030
Nature. 1983 Jul 28-Aug 3;304(5924):368-71
pubmed: 6877358