dc.contributor.author |
Fujiki K. |
|
dc.contributor.author |
Yano S. |
|
dc.contributor.author |
Ito T. |
|
dc.contributor.author |
Kumagai Y. |
|
dc.contributor.author |
Murakami Y. |
|
dc.contributor.author |
Kamigaito O. |
|
dc.contributor.author |
Haba H. |
|
dc.contributor.author |
Tanaka K. |
|
dc.date.accessioned |
2018-09-19T22:33:08Z |
|
dc.date.available |
2018-09-19T22:33:08Z |
|
dc.date.issued |
2017 |
|
dc.identifier.uri |
https://dspace.kpfu.ru/xmlui/handle/net/145305 |
|
dc.description.abstract |
© 2017 The Author(s).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. |
|
dc.title |
A One-Pot Three-Component Double-Click Method for Synthesis of [<sup>67</sup>Cu]-Labeled Biomolecular Radiotherapeutics |
|
dc.type |
Article |
|
dc.relation.ispartofseries-issue |
1 |
|
dc.relation.ispartofseries-volume |
7 |
|
dc.collection |
Публикации сотрудников КФУ |
|
dc.source.id |
SCOPUS-2017-7-1-SID85019420153 |
|