Development of Fibroblast Activation Protein-Targeted Radiotracers with Improved Tumor Retention.
Animals
Cell Line
Cell Line, Tumor
Chelating Agents
/ pharmacology
Endopeptidases
Gelatinases
/ chemistry
Humans
Image Processing, Computer-Assisted
Membrane Proteins
/ chemistry
Mice
Mice, Inbred BALB C
Mice, Nude
Neoplasm Transplantation
Neoplasms
/ diagnostic imaging
Positron-Emission Tomography
Protein Binding
Quinolines
/ chemistry
Radiopharmaceuticals
/ pharmacokinetics
Serine Endopeptidases
/ chemistry
Solvents
Treatment Outcome
FAP inhibitor
PET/CT
fibroblast activation protein
theranostics
tracer development
Journal
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
ISSN: 1535-5667
Titre abrégé: J Nucl Med
Pays: United States
ID NLM: 0217410
Informations de publication
Date de publication:
10 2019
10 2019
Historique:
received:
05
12
2018
accepted:
04
03
2019
pubmed:
10
3
2019
medline:
14
4
2020
entrez:
10
3
2019
Statut:
ppublish
Résumé
Cancer-associated fibroblasts constitute a vital subpopulation of the tumor stroma and are present in more than 90% of epithelial carcinomas. The overexpression of the serine protease fibroblast activation protein (FAP) allows a selective targeting of a variety of tumors by inhibitor-based radiopharmaceuticals (FAPIs). Of these compounds, FAPI-04 has been recently introduced as a theranostic radiotracer and demonstrated high uptake into different FAP-positive tumors in cancer patients. To enable the delivery of higher doses, thereby improving the outcome of a therapeutic application, several FAPI variants were designed to further increase tumor uptake and retention of these tracers.
Identifiants
pubmed: 30850501
pii: jnumed.118.224469
doi: 10.2967/jnumed.118.224469
pmc: PMC6785792
doi:
Substances chimiques
Chelating Agents
0
FAPI-46
0
Membrane Proteins
0
Quinolines
0
Radiopharmaceuticals
0
Solvents
0
Endopeptidases
EC 3.4.-
Serine Endopeptidases
EC 3.4.21.-
fibroblast activation protein alpha
EC 3.4.21.-
Gelatinases
EC 3.4.24.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1421-1429Informations de copyright
© 2019 by the Society of Nuclear Medicine and Molecular Imaging.
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