| Title : Next generation fibroblast activation protein (FAP) targeting PET tracers - The tetrazine ligation allows an easy and convenient way to (18)F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines - Poulie_2023_Eur.J.Med.Chem_262_115862 |
| Author(s) : Poulie CBM , Shalgunov V , Elvas F , Van Rymenant Y , Moon ES , Battisti UM , De Loose J , De Meester I , Rosch F , Van der Veken P , Herth MM |
| Ref : Eur Journal of Medicinal Chemistry , 262 :115862 , 2023 |
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Abstract :
Small-molecular fibroblast activation protein inhibitor (FAPI)-based tracer have been shown to be promising Positron Emission Tomography (PET) (68)Ga-labeled radiopharmaceuticals to image a variety of tumors including pancreatic, breast, and colorectal cancers, among others. In this study, we developed a novel (18)F-labeled FAPI derivative. [(18)F]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. [(18)F]6 was excreted via the liver. Overall, [(18)F]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. |
| PubMedSearch : Poulie_2023_Eur.J.Med.Chem_262_115862 |
| PubMedID: 37883899 |
Poulie CBM, Shalgunov V, Elvas F, Van Rymenant Y, Moon ES, Battisti UM, De Loose J, De Meester I, Rosch F, Van der Veken P, Herth MM (2023)
Next generation fibroblast activation protein (FAP) targeting PET tracers - The tetrazine ligation allows an easy and convenient way to (18)F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines
Eur Journal of Medicinal Chemistry
262 :115862
Poulie CBM, Shalgunov V, Elvas F, Van Rymenant Y, Moon ES, Battisti UM, De Loose J, De Meester I, Rosch F, Van der Veken P, Herth MM (2023)
Eur Journal of Medicinal Chemistry
262 :115862