Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX.
Adenocarcinoma
/ diagnostic imaging
Animals
Antigens, Neoplasm
/ analysis
Biomarkers, Tumor
/ analysis
Carbonic Anhydrase IX
/ analysis
Cattle
Cell Line, Tumor
Click Chemistry
Colorectal Neoplasms
/ diagnostic imaging
Drug Stability
Fluorine Radioisotopes
Humans
Isotope Labeling
Mice
Peptides
/ chemical synthesis
Positron-Emission Tomography
Radiopharmaceuticals
/ chemical synthesis
Serum
/ metabolism
Tomography, X-Ray Computed
Triazoles
/ chemical synthesis
Tumor Hypoxia
/ physiology
(18)F-labeling
Carbonic anhydrase IX
PET imaging
Peptide
Tumor hypoxia
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 03 2019
01 03 2019
Historique:
received:
19
10
2018
revised:
12
01
2019
accepted:
16
01
2019
pubmed:
27
1
2019
medline:
15
1
2020
entrez:
27
1
2019
Statut:
ppublish
Résumé
Carbonic anhydrase IX (CA IX) is the first carbonic anhydrase found to be associated with cancer that is over-expressed in a variety of human solid tumors. As a surrogate marker for hypoxia, the expression of CA IX is strongly upregulated in hypoxic tumors by hypoxia and hypoxia-inducible factor 1a (HIF-1a). In our pursuit of a CA IX-specific PET probe, we designed and synthesized a peptide-based CA IX imaging probe by the efficient click reaction of 1,3-dipolar cycloaddition of terminal alkynes and organic azides. The probe
Identifiants
pubmed: 30683555
pii: S0968-0896(18)31659-6
doi: 10.1016/j.bmc.2019.01.014
pii:
doi:
Substances chimiques
Antigens, Neoplasm
0
Biomarkers, Tumor
0
Fluorine Radioisotopes
0
Peptides
0
Radiopharmaceuticals
0
Triazoles
0
CA9 protein, human
EC 4.2.1.1
Carbonic Anhydrase IX
EC 4.2.1.1
Fluorine-18
GZ5I74KB8G
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
785-789Informations de copyright
Copyright © 2019 Elsevier Ltd. All rights reserved.