TY - JOUR
T1 - Relevance of Palladium to Radiopharmaceutical Development Considering Enhanced Coordination Properties of TE1PA
AU - Pineau, Julie
AU - Lima, Luís M.P.
AU - Platas-Iglesias, Carlos
AU - Zeevaart, Jan Rijn
AU - Driver, Cathryn H.S.
AU - Le Bris, Nathalie
AU - Tripier, Raphaël
N1 - Funding Information:
R.T. and N.L.B. acknowledge the Ministère de l′Enseignement Supérieur et de la Recherche and the Centre National de la Recherche Scientifique. J.P. is grateful to the Ligue contre le Cancer, the MAC‐group (UBO) and the University of Cape Town for her PhD fellowship; C.H.S.D thanks the Technology Innovation Agency (TIA) seed fund implemented through the South African Nuclear Energy Corporation for financial support. C.P.‐I. thanks Centro de Supercomputación de Galicia for providing access to computing facilities. L.M.P.L was financially supported by Project LISBOA‐01‐0145‐FEDER‐007660 (Microbiologia Molecular, Estrutural e Celular), funded by FEDER funds through COMPETE2020 ‐ Programa Operacional Competitividade e Internacionalização (POCI) and by national funds through FCT ‐ Fundação para a Ciência e a Tecnologia.
Publisher Copyright:
© 2022 The Authors. Chemistry - A European Journal published by Wiley-VCH GmbH.
PY - 2022
Y1 - 2022
N2 - The limited use of palladium-103 and -109 radionuclides for molecular radiotherapy is surely due to the lack of appropriate ligands capable of fulfilling all criteria required for application in nuclear medicine. Furthermore, the thermodynamic properties of these complexes in solution remain difficult to establish. The challenge is compounded when considering that radiolabeling of compounds for translation to clinical trials requires fast complexation. Thus, the coordination of Pd(II) and 103/109Pd-nuclides is a huge challenge in terms of molecular design and physicochemical characterization. Herein, we report a comprehensive study highlighting TE1PA, a monopicolinate cyclam – already established in nuclear imaging with 64Cu-PET (positron emission tomography) imaging tracers – as a highly relevant chelator for natural Pd and subsequently 109Pd-nuclide. The structural, thermodynamic, kinetic and radiolabeling studies of Pd(II) with TE1PA, as well as the comparison of this complex with three structurally related derivatives, support palladium-TE1PA radiopharmaceuticals as leading candidates for targeted nuclear medicine.
AB - The limited use of palladium-103 and -109 radionuclides for molecular radiotherapy is surely due to the lack of appropriate ligands capable of fulfilling all criteria required for application in nuclear medicine. Furthermore, the thermodynamic properties of these complexes in solution remain difficult to establish. The challenge is compounded when considering that radiolabeling of compounds for translation to clinical trials requires fast complexation. Thus, the coordination of Pd(II) and 103/109Pd-nuclides is a huge challenge in terms of molecular design and physicochemical characterization. Herein, we report a comprehensive study highlighting TE1PA, a monopicolinate cyclam – already established in nuclear imaging with 64Cu-PET (positron emission tomography) imaging tracers – as a highly relevant chelator for natural Pd and subsequently 109Pd-nuclide. The structural, thermodynamic, kinetic and radiolabeling studies of Pd(II) with TE1PA, as well as the comparison of this complex with three structurally related derivatives, support palladium-TE1PA radiopharmaceuticals as leading candidates for targeted nuclear medicine.
KW - complexation
KW - cyclam
KW - cyclam monopicolinate
KW - palladium(II)
KW - palladium-109
KW - radiolabeling
UR - https://www.scopus.com/pages/publications/85131589895
U2 - 10.1002/chem.202200942
DO - 10.1002/chem.202200942
M3 - Article
C2 - 35560962
AN - SCOPUS:85131589895
SN - 0947-6539
JO - Chemistry - A European Journal
JF - Chemistry - A European Journal
ER -