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

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

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

In: European Journal of Medicinal Chemistry, Vol. 262, 115862, 2023.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Poulie, CBM, Shalgunov, V, Elvas, F, Van Rymenant, Y, Moon, ES, Battisti, UM, De Loose, J, De Meester, I, Rösch, 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 18F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines', European Journal of Medicinal Chemistry, vol. 262, 115862. https://doi.org/10.1016/j.ejmech.2023.115862

APA

Poulie, C. B. M., Shalgunov, V., Elvas, F., Van Rymenant, Y., Moon, E. S., Battisti, U. M., De Loose, J., De Meester, I., Rösch, F., Van Der Veken, P., & Herth, M. M. (2023). 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. European Journal of Medicinal Chemistry, 262, [115862]. https://doi.org/10.1016/j.ejmech.2023.115862

Vancouver

Poulie CBM, Shalgunov V, Elvas F, Van Rymenant Y, Moon ES, Battisti UM et al. 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. European Journal of Medicinal Chemistry. 2023;262. 115862. https://doi.org/10.1016/j.ejmech.2023.115862

Author

Poulie, Christian B.M. ; Shalgunov, Vladimir ; Elvas, Filipe ; Van Rymenant, Yentl ; Moon, Euy Sung ; Battisti, Umberto Maria ; De Loose, Joni ; De Meester, Ingrid ; Rösch, Frank ; Van Der Veken, Pieter ; Herth, Matthias M. / 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. In: European Journal of Medicinal Chemistry. 2023 ; Vol. 262.

Bibtex

@article{017f9c0c4aeb4d07ac236902d3f7b480,
title = "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",
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.",
keywords = "FAPI, Fluorine-18, PET, Tetrazine ligation, Theranostics",
author = "Poulie, {Christian B.M.} and Vladimir Shalgunov and Filipe Elvas and {Van Rymenant}, Yentl and Moon, {Euy Sung} and Battisti, {Umberto Maria} and {De Loose}, Joni and {De Meester}, Ingrid and Frank R{\"o}sch and {Van Der Veken}, Pieter and Herth, {Matthias M.}",
note = "Publisher Copyright: {\textcopyright} 2023 The Authors",
year = "2023",
doi = "10.1016/j.ejmech.2023.115862",
language = "English",
volume = "262",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson",

}

RIS

TY - JOUR

T1 - Next generation fibroblast activation protein (FAP) targeting PET tracers 

T2 - 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 - Publisher Copyright: © 2023 The Authors

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.

KW - FAPI

KW - Fluorine-18

KW - PET

KW - Tetrazine ligation

KW - Theranostics

U2 - 10.1016/j.ejmech.2023.115862

DO - 10.1016/j.ejmech.2023.115862

M3 - Journal article

C2 - 37883899

AN - SCOPUS:85174564344

VL - 262

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

M1 - 115862

ER -

ID: 373617240