In Vivo Albumin‐Binding of a C ‐Functionalized Cyclam Platform for 64 Cu‐PET/CT Imaging in Breast Cancer Model
| Autor: | Thomas Le Bihan, Cathryn H.S. Driver, Raphaël Tripier, Thomas Ebenhan, Nathalie Le Bris, Jan Rijn Zeevaart |
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| Přispěvatelé: | Chimie, Electrochimie Moléculaires et Chimie Analytique (CEMCA), Institut Brestois Santé Agro Matière (IBSAM), Université de Brest (UBO)-Université de Brest (UBO)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), South African Nuclear Energy Corporation Radiochemistry and NuMeRI PreClinical Imaging Facility (SANECR-NuMeRi_PCIF) |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Biodistribution
[CHIM.THER]Chemical Sciences/Medicinal Chemistry 01 natural sciences Biochemistry chemistry.chemical_compound TE3A Breast cancer In vivo Drug Discovery Cyclam Radioligand medicine [CHIM]Chemical Sciences 64-Cu PET General Pharmacology Toxicology and Pharmaceutics Pharmacology Bioconjugation 010405 organic chemistry tumor targeting Organic Chemistry Albumin EPR effect medicine.disease Blood proteins 0104 chemical sciences 3. Good health 010404 medicinal & biomolecular chemistry chemistry Cancer research Molecular Medicine |
| Zdroj: | ChemMedChem ChemMedChem, Wiley-VCH Verlag, 2020, ⟨10.1002/cmdc.202000800⟩ |
| ISSN: | 1860-7179 1860-7187 |
| Popis: | International audience; An improved glucose‐chelator‐albumin bioconjugate (GluCAB) derivative, GluCAB‐2Mal, has been synthesized and studied for in vivo 64Cu‐PET/CT imaging in breast cancer mice models together with its first‐generation analogue GluCAB‐1Mal. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [64Cu]Cu‐GluCAB‐2Mal (99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [64Cu]Cu‐GluCAB‐2Mal and previous‐generation [64Cu]Cu‐GluCAB‐1Mal encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [64Cu]Cu‐GluCAB‐2Mal was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [64Cu]Cu‐Glu‐CAB‐2Mal. |
| Databáze: | OpenAIRE |
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