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Porphyrin-Based Brain Tumor-Targeting Agents: [ 64 Cu]Cu-porphyrin and [ 64 Cu]Cu-TDAP.
- Source :
-
Molecular pharmaceutics [Mol Pharm] 2023 Nov 06; Vol. 20 (11), pp. 5856-5864. Date of Electronic Publication: 2023 Oct 18. - Publication Year :
- 2023
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Abstract
- The aim of this study is to evaluate a radioactive metal complex platform for brain tumor targeting. Herein, we introduce a new porphyrin derivative, 5,10,15,20-(tetra- N , N -dimethyl-4-aminophenyl)porphyrin (TDAP), in which four N , N -dimethyl-4- p -phenylenediamine (DMPD) moieties are conjugated to the porphyrin labeled with the radiometal <superscript>64</superscript> Cu. DMPD affected the pharmacokinetics of porphyrin in terms of retention time in vivo and tumor-targeting ability relative to those of unmodified porphyrin. [ <superscript>64</superscript> Cu]Cu-TDAP showed stronger enhancement than [ <superscript>64</superscript> Cu]Cu-porphyrin in U87MG glioblastoma cells, especially in the cytoplasm and nucleus, indicating its tumor-targeting properties and potential use as a therapeutic agent. In the subcutaneous and orthotopic models of brain-tumor-bearing mice, [ <superscript>64</superscript> Cu]Cu-TDAP was clearly visualized in the tumor site via positron emission tomography imaging and showed a tumor-to-brain ratio as high as 13. [ <superscript>64</superscript> Cu]Cu-TDAP deserves attention as a new diagnostic agent that is suitable for the early diagnosis and treatment of brain tumors.
Details
- Language :
- English
- ISSN :
- 1543-8392
- Volume :
- 20
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Molecular pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 37851927
- Full Text :
- https://doi.org/10.1021/acs.molpharmaceut.3c00704