2021
DOI: 10.3390/cancers13225744
|View full text |Cite
|
Sign up to set email alerts
|

Radioligands Targeting Fibroblast Activation Protein (FAP)

Abstract: Targeting fibroblast activation protein (FAP) in cancer-associated fibroblasts (CAFs) has attracted significant attention in nuclear medicine. Since these cells are present in most cancerous tissues and FAP is rarely expressed in healthy tissues, anti-FAP tracers have a potential as pan-tumor agents. Compared to the standard tumor tracer [18F]FDG, these tracers show better tumor-to-background ratios (TBR) in many indications. Unlike [18F]FDG, FAP-targeted tracers do not require exhausting preparations, such as… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1
1

Citation Types

0
24
0

Year Published

2022
2022
2024
2024

Publication Types

Select...
8
1

Relationship

0
9

Authors

Journals

citations
Cited by 42 publications
(24 citation statements)
references
References 48 publications
0
24
0
Order By: Relevance
“…FAP is an atypical type II transmembrane serine protease with dipeptidyl peptidase (DPP) and endopeptidase activities [ 8 ]. FAP is highly expressed on activated fibroblasts, and fibroblasts undergo dimerization and glycosylation when activated [ 9 ]. In adult tissues, activated FAP almost only exists in the stroma of wound healing, fibrosis, and malignant tumors [ 10 ].…”
Section: Fibroblast Activation Protein (Fap) and Fapimentioning
confidence: 99%
“…FAP is an atypical type II transmembrane serine protease with dipeptidyl peptidase (DPP) and endopeptidase activities [ 8 ]. FAP is highly expressed on activated fibroblasts, and fibroblasts undergo dimerization and glycosylation when activated [ 9 ]. In adult tissues, activated FAP almost only exists in the stroma of wound healing, fibrosis, and malignant tumors [ 10 ].…”
Section: Fibroblast Activation Protein (Fap) and Fapimentioning
confidence: 99%
“…Researchers of the University of Heidelberg were the first to report on FAP inhibitors (FAPIs) for radionuclide theranostics. A panel of radiolabeled FAPIs were developed by this group, of which FAPI-04, FAPI-46, and FAPI-74 were proved to be the most successful in clinical imaging studies [92][93][94]. PET/ CT scans with FAPI-04 allowed for the diagnosis of 28 different tumor types in 80 patients (Fig.…”
Section: Cancer-associated Fibroblastsmentioning
confidence: 99%
“…It is an important marker of cancer-associated fibroblasts that appears to contribute to some of their tumor-promoting activities [78]. After the identification of the FAP inhibitor (FAPi) lead molecule UAMC-1110 [79], many FAP-targeting imaging tools based on the same quinoline scaffold were designed for theranostic applications in a variety of cancers [80,81]. For that purpose, the use of the squaramide motif to anchor a chelating moiety on a vector molecule has been exemplified with FAPi compounds: the team of Frank Rösch synthesized and evaluated a DATA 5m -SA-FAPi derivative in comparison with its DOTA analogue [82].…”
Section: Fibroblast Activation Protein Inhibitorsmentioning
confidence: 99%