Imaging of the Glucose-Dependent Insulinotropic Polypeptide Receptor Using a Novel Radiolabeled Peptide Rationally Designed Based on Endogenous GIP and Synthetic Exendin-4 Sequences.

GIPR PET insulinoma neuroendocrine tumors

Journal

Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453

Informations de publication

Date de publication:
31 Dec 2022
Historique:
received: 22 11 2022
revised: 15 12 2022
accepted: 23 12 2022
entrez: 21 1 2023
pubmed: 22 1 2023
medline: 22 1 2023
Statut: epublish

Résumé

Imaging and radiotherapy targeting the glucose-dependent insulinotropic polypeptide receptor (GIPR) could potentially benefit the management of neuroendocrine neoplasms (NENs), complementing clinically established radiopharmaceuticals. The aim of this study was to evaluate a GIPR-targeting positron emission tomography (PET) radioligand with receptor-specific binding, fast blood clearance, and low liver background uptake. The peptide DOTA-bioconjugate, C803-GIP, was developed based on the sequence of the endogenous GIP(1-30) and synthetic exendin-4 peptides with selective amino acid mutations to combine their specificity for the GIPR and in vivo stability, respectively. The

Identifiants

pubmed: 36678558
pii: ph16010061
doi: 10.3390/ph16010061
pmc: PMC9864903
pii:
doi:

Types de publication

Journal Article

Langues

eng

Références

J Labelled Comp Radiopharm. 2015 Mar;58(3):99-121
pubmed: 25689590
J Clin Endocrinol Metab. 2012 Feb;97(2):482-8
pubmed: 22112810
Sci Rep. 2020 Oct 7;10(1):16758
pubmed: 33028880
Lancet Diabetes Endocrinol. 2013 Oct;1(2):115-22
pubmed: 24622317
Surgery. 2013 Dec;154(6):1206-13; discussion 1214
pubmed: 24238043
Peptides. 2020 Mar;125:170229
pubmed: 31857104
N Engl J Med. 2008 Aug 14;359(7):766-8
pubmed: 18703486
Regul Pept. 2013 Feb 10;181:17-21
pubmed: 23318502
Pharmacol Rev. 2003 Mar;55(1):167-94
pubmed: 12615957
J Nucl Med. 2015 Apr;56(4):613-5
pubmed: 25698785
Neuroendocrinology. 2015;101(1):1-17
pubmed: 25228173
Semin Oncol. 2010 Dec;37(6):662-79
pubmed: 21167384
Mol Pharmacol. 2010 Apr;77(4):547-58
pubmed: 20061446
J Med Chem. 2017 May 25;60(10):4293-4303
pubmed: 28448133
Diabetes. 2021 Apr;70(4):842-853
pubmed: 33547046
Med Chem. 2011 Sep;7(5):345-79
pubmed: 21711223
Hepatobiliary Surg Nutr. 2020 Aug;9(4):440-451
pubmed: 32832495
J Nucl Med. 2014 Jun;55(6):976-82
pubmed: 24744444
Sci Rep. 2018 Feb 13;8(1):2948
pubmed: 29440684
Biochem Biophys Res Commun. 2004 Jul 30;320(3):900-6
pubmed: 15240133
J Clin Endocrinol Metab. 2014 May;99(5):1519-24
pubmed: 24512490
J Nucl Med. 2013 Mar;54(3):364-72
pubmed: 23297077
EJNMMI Res. 2022 Apr 8;12(1):19
pubmed: 35394238
Theranostics. 2013 Dec 10;4(1):47-80
pubmed: 24396515
N Engl J Med. 2017 Jan 12;376(2):125-135
pubmed: 28076709
J Surg Res. 2014 Aug;190(2):587-93
pubmed: 24565507
EJNMMI Res. 2019 Feb 15;9(1):17
pubmed: 30771019
J Nucl Med. 2009 Mar;50(3):477-84
pubmed: 19258258

Auteurs

Irina Velikyan (I)

Science for Life Laboratory, Department of Medicinal Chemistry, Uppsala University, SE-751 83 Uppsala, Sweden.
PET Centre, Centre for Medical Imaging, Uppsala University Hospital, SE-751 85 Uppsala, Sweden.

Martin Bossart (M)

R&D Research Platform, Integrated Drug Discovery, Sanofi, 65929 Frankfurt, Germany.

Torsten Haack (T)

R&D Research Platform, Integrated Drug Discovery, Sanofi, 65929 Frankfurt, Germany.

Iina Laitinen (I)

Global Imaging, Sanofi, 65929 Frankfurt, Germany.

Sergio Estrada (S)

Science for Life Laboratory, Department of Medicinal Chemistry, Uppsala University, SE-751 83 Uppsala, Sweden.

Lars Johansson (L)

Antaros Medical AB, SE-431 53 Mölndal, Sweden.

Stefan Pierrou (S)

Antaros Medical AB, SE-431 53 Mölndal, Sweden.

Michael Wagner (M)

R&D Research Platform, Integrated Drug Discovery, Sanofi, 65929 Frankfurt, Germany.

Olof Eriksson (O)

Science for Life Laboratory, Department of Medicinal Chemistry, Uppsala University, SE-751 83 Uppsala, Sweden.
Antaros Medical AB, SE-431 53 Mölndal, Sweden.

Classifications MeSH