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A One-Pot Three-Component Double-Click Method for Synthesis of [67Cu]-Labeled Biomolecular Radiotherapeutics
- Source :
- Scientific Reports, Scientific Reports, Vol 7, Iss 1, Pp 1-9 (2017)
- Publication Year :
- 2017
- Publisher :
- Springer Science and Business Media LLC, 2017.
-
Abstract
- A one-pot three-component double-click process for preparing tumor-targeting agents for cancer radiotherapy is described here. By utilizing DOTA (or NOTA) containing tetrazines and the TCO-substituted aldehyde, the two click reactions, the tetrazine ligation (an inverse electron-demand Diels-Alder cycloaddition) and the RIKEN click (a rapid 6π-azaelectrocyclization), could simultaneously proceed under mild conditions to afford covalent attachment of the metal chelator DOTA or NOTA to biomolecules such as to albumin and anti-IGSF4 antibody without altering their activities. Subsequently, radiolabeling of DOTA- or NOTA-attached albumin and anti-IGSF4 antibody (an anti-tumor-targeting antibody) with [67Cu], a β−-emitting radionuclide, could be achieved in a highly efficient manner via a simple chelation with DOTA proving to be a more superior chelator than NOTA. Our work provides a new and operationally simple method for introducing the [67Cu] isotope even in large quantities to biomolecules, thereby representing an important process for preparations of clinically relevant tumor-targeting agents for radiotherapy.
- Subjects :
- Science
010402 general chemistry
01 natural sciences
Aldehyde
Metal Chelator
Article
Antibodies
Tetrazine
chemistry.chemical_compound
Albumins
Organometallic Compounds
Humans
DOTA
Chelation
chemistry.chemical_classification
Multidisciplinary
Molecular Structure
010405 organic chemistry
Biomolecule
Combinatorial chemistry
Cycloaddition
0104 chemical sciences
HEK293 Cells
Copper Radioisotopes
chemistry
Covalent bond
Isotope Labeling
Medicine
Click Chemistry
Radiopharmaceuticals
Subjects
Details
- ISSN :
- 20452322
- Volume :
- 7
- Database :
- OpenAIRE
- Journal :
- Scientific Reports
- Accession number :
- edsair.doi.dedup.....6087f2c0a7f98ccf9c74ee1eb76b0a21