Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA
DATA5m
DOTA
FAP
Gallium-68
HT-29
PREP
Squaramide
Squaric acid
Journal
EJNMMI radiopharmacy and chemistry
ISSN: 2365-421X
Titre abrégé: EJNMMI Radiopharm Chem
Pays: England
ID NLM: 101714628
Informations de publication
Date de publication:
29 Jul 2020
29 Jul 2020
Historique:
received:
02
06
2020
accepted:
15
07
2020
entrez:
31
7
2020
pubmed:
31
7
2020
medline:
31
7
2020
Statut:
epublish
Résumé
Fibroblast activation protein (FAP) is a proline selective serine protease that is overexpressed in tumor stroma and in lesions of many other diseases that are characterized by tissue remodeling. In 2014, a most potent FAP-inhibitor (referred to as UAMC1110) with low nanomolar FAP-affinity and high selectivity toward related enzymes such as prolyl oligopeptidase (PREP) and the dipeptidyl-peptidases (DPPs): DPP4, DPP8/9 and DPP2 were developed. This inhibitor has been adopted recently by other groups to create radiopharmaceuticals by coupling bifunctional chelator-linker systems. Here, we report squaric acid (SA) containing bifunctional DATA [ In this work, novel PET radiotracers targeting fibroblast activation protein were synthesized and biochemically investigated. Critical substructures of the novel compounds are a squaramide linker unit derived from the basic motif of squaric acid, DOTA and DATA
Sections du résumé
BACKGROUND
BACKGROUND
Fibroblast activation protein (FAP) is a proline selective serine protease that is overexpressed in tumor stroma and in lesions of many other diseases that are characterized by tissue remodeling. In 2014, a most potent FAP-inhibitor (referred to as UAMC1110) with low nanomolar FAP-affinity and high selectivity toward related enzymes such as prolyl oligopeptidase (PREP) and the dipeptidyl-peptidases (DPPs): DPP4, DPP8/9 and DPP2 were developed. This inhibitor has been adopted recently by other groups to create radiopharmaceuticals by coupling bifunctional chelator-linker systems. Here, we report squaric acid (SA) containing bifunctional DATA
RESULTS
RESULTS
[
CONCLUSION
CONCLUSIONS
In this work, novel PET radiotracers targeting fibroblast activation protein were synthesized and biochemically investigated. Critical substructures of the novel compounds are a squaramide linker unit derived from the basic motif of squaric acid, DOTA and DATA
Identifiants
pubmed: 32728930
doi: 10.1186/s41181-020-00102-z
pii: 10.1186/s41181-020-00102-z
pmc: PMC7391456
doi:
Types de publication
Journal Article
Langues
eng
Pagination
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