Evaluation of a Bispidine‐Based Chelator for Gallium‐68 and of the Porphyrin Conjugate as PET/PDT Theranostic Agent
| Autor: | Steven Y. Yap, Huguette Savoie, Aline Nonat, Ross W. Boyle, Thomas W. Price, Graeme J. Stasiuk, Raphaël Gillet, Loïc J. Charbonnière |
|---|---|
| Přispěvatelé: | University of Hull, Institut Pluridisciplinaire Hubert Curien (IPHC), Université de Strasbourg (UNISTRA)-Institut National de Physique Nucléaire et de Physique des Particules du CNRS (IN2P3)-Centre National de la Recherche Scientifique (CNRS) |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Porphyrins
theranostic chemistry.chemical_element Gallium Gallium Radioisotopes Conjugated system 010402 general chemistry Ligands 01 natural sciences Catalysis Theranostic Nanomedicine chemistry.chemical_compound gallium-68 medicine Humans [CHIM]Chemical Sciences Chelation bispidine radiochemistry Chelating Agents medicine.diagnostic_test 010405 organic chemistry Organic Chemistry General Chemistry Ligand (biochemistry) Bridged Bicyclo Compounds Heterocyclic Combinatorial chemistry Porphyrin 3. Good health 0104 chemical sciences chemistry Positron emission tomography Positron-Emission Tomography Bifunctional chelator porphyrin Conjugate |
| Zdroj: | Chemistry-A European Journal Chemistry-A European Journal, Wiley-VCH Verlag, 2020, ⟨10.1002/chem.201905776⟩ Price, T, Yap, S, Gillet, R, Savoie, H, Charbonnière, L, Boyle, R, Nonat, A & Stasiuk, G J 2020, ' Evaluation of a bispidine-based chelator for gallium-68 and of the porphyrin conjugate as PET/PDT theranostic agent ', Chemistry (Weinheim an der Bergstrasse, Germany), vol. 26, no. 34, pp. 7602-7608 . https://doi.org/10.1002/chem.201905776 |
| ISSN: | 0947-6539 1521-3765 |
| DOI: | 10.1002/chem.201905776⟩ |
| Popis: | International audience; In this study a bispidine ligand has been applied to the complexation of gallium(III) and radiolabelled with gallium-68 for the first time. Despite its 5-coordinate nature, the resulting complex is stable in serum for over two hours, demonstrating a ligand system well matched to the imaging window of gallium-68 positron emission tomography (PET). To show the versatility of the bispidine ligand and its potential use in PET, the bifunctional chelator was conjugated to a porphyrin, producing a PET/PDT-theranostic, which showed the same level of stability to serum as the non-conjugated gallium-68 complex. The PET/PDT complex killed >90 % of HT-29 cells upon light irradiation at 50 mu m. This study shows bispidines have the versatility to be used as a ligand system for gallium-68 in PET. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text