Next generation fibroblast activation protein (FAP) targeting PET tracers - The tetrazine ligation allows an easy and convenient way to 18F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines

Christian B M Poulie, Vladimir Shalgunov, Filipe Elvas, Yentl Van Rymenant, Euy-Sung Moon, Umberto Maria Battisti, Joni De Loose, Ingrid De Meester, Frank Rösch, Pieter Van Der Veken, Matthias M Herth*

*Corresponding author af dette arbejde
4 Citationer (Scopus)

Abstract

Small-molecular fibroblast activation protein inhibitor (FAPI)-based tracer have been shown to be promising Positron Emission Tomography (PET) 68Ga-labeled radiopharmaceuticals to image a variety of tumors including pancreatic, breast, and colorectal cancers, among others. In this study, we developed a novel 18F-labeled FAPI derivative. [18F]6 was labeled using a synthon approach based on the tetrazine ligation. It showed subnanomolar affinity for the FAP protein and a good selectivity profile against known off-target proteases. Small animal PET studies revealed high tumor uptake and good target-to-background ratios. [18F]6 was excreted via the liver. Overall, [18F]6 showed promising characteristics to be used as a PET tracer and could serve as a lead for further development of halogen-based theranostic FAPI radiopharmaceuticals.

OriginalsprogEngelsk
Artikelnummer115862
TidsskriftEuropean Journal of Medicinal Chemistry
Vol/bind262
Antal sider10
ISSN0223-5234
DOI
StatusUdgivet - 2023

Fingeraftryk

Dyk ned i forskningsemnerne om 'Next generation fibroblast activation protein (FAP) targeting PET tracers - The tetrazine ligation allows an easy and convenient way to 18F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines'. Sammen danner de et unikt fingeraftryk.

Citationsformater