TY - JOUR
T1 - 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
AU - Poulie, Christian B M
AU - Shalgunov, Vladimir
AU - Elvas, Filipe
AU - Van Rymenant, Yentl
AU - Moon, Euy-Sung
AU - Battisti, Umberto Maria
AU - De Loose, Joni
AU - De Meester, Ingrid
AU - Rösch, Frank
AU - Van Der Veken, Pieter
AU - Herth, Matthias M
N1 - Copyright © 2023 The Authors. Published by Elsevier Masson SAS.. All rights reserved.
PY - 2023
Y1 - 2023
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85174564344&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2023.115862
DO - 10.1016/j.ejmech.2023.115862
M3 - Journal article
C2 - 37883899
SN - 0223-5234
VL - 262
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
M1 - 115862
ER -