Development of Novel
A549 Cells
Animals
Female
HEK293 Cells
Heterocyclic Compounds, 1-Ring
/ chemistry
Humans
Indium Radioisotopes
/ chemistry
Mice
Mice, Nude
Neoplasm Proteins
/ metabolism
Neoplasms
/ drug therapy
Radiopharmaceuticals
/ chemistry
Receptors, G-Protein-Coupled
/ metabolism
Urotensins
/ chemistry
Xenograft Model Antitumor Assays
111Indium-DOTA-peptide analogues
UT receptor
carcinoma
radiolabelling
urotensin II
Journal
Biomolecules
ISSN: 2218-273X
Titre abrégé: Biomolecules
Pays: Switzerland
ID NLM: 101596414
Informations de publication
Date de publication:
19 03 2020
19 03 2020
Historique:
received:
11
03
2020
revised:
17
03
2020
accepted:
18
03
2020
entrez:
25
3
2020
pubmed:
25
3
2020
medline:
18
3
2021
Statut:
epublish
Résumé
Overexpression of G protein-coupled receptors (GPCRs) in tumours is widely used to develop GPCR-targeting radioligands for solid tumour imaging in the context of diagnosis and even treatment. The human vasoactive neuropeptide urotensin II (hUII), which shares structural analogies with somatostatin, interacts with a single high affinity GPCR named UT. High expression of UT has been reported in several types of human solid tumours from lung, gut, prostate, or breast, suggesting that UT is a valuable novel target to design radiolabelled hUII analogues for cancer diagnosis. In this study, two original urotensinergic analogues were first conjugated to a DOTA chelator via an aminohexanoic acid (Ahx) hydrocarbon linker and then -hUII and DOTA-urantide, complexed to the radioactive metal indium isotope to successfully lead to radiolabelled DOTA-Ahx-hUII and DOTA-Ahx-urantide. The
Identifiants
pubmed: 32204509
pii: biom10030471
doi: 10.3390/biom10030471
pmc: PMC7175314
pii:
doi:
Substances chimiques
Heterocyclic Compounds, 1-Ring
0
Indium Radioisotopes
0
Neoplasm Proteins
0
Radiopharmaceuticals
0
Receptors, G-Protein-Coupled
0
UTS2R protein, human
0
Urotensins
0
1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
1HTE449DGZ
urotensin II
9047-55-6
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Ligue Normandie contre le Cancer
ID : 2016
Pays : International
Organisme : Inserm
ID : 2016-2018
Pays : International
Organisme : Géfluc
ID : 2017
Pays : International
Organisme : University Rouen Normandie
ID : 2018
Pays : International
Organisme : Region Normandie and FEDER
ID : 2016
Pays : International
Déclaration de conflit d'intérêts
The authors declare no conflict of interest.
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