Dr Louis Allott Louis.Allott@hull.ac.uk
Lecturer in Translational Radiopharmaceutics
Dr Louis Allott Louis.Allott@hull.ac.uk
Lecturer in Translational Radiopharmaceutics
Cen Chen
Marta Braga
Sau Fung Jacob Leung
Ning Wang
Chris Barnes
Diana Brickute
Laurence Carroll
Eric O. Aboagye
We have exemplified a pretargeted approach to interrogate hypoxia in live cells using radioactive bioorthogonal inverse electron demand Diels–Alder (IEDDA) “click” chemistry. Our novel 18F-tetrazine probe ([18F]FB-Tz) and 2-nitroimidazole-based TCO targeting molecule (8) showed statistically significant (P < 0.0001) uptake in hypoxic cells (ca. 90 %ID per mg) vs. normoxic cells (< 10 %ID per mg) in a 60 min incubation of [18F]FB-Tz. This is the first time that an intracellularly targeted small-molecule for IEDDA “click” has been used in conjunction with a radioactive reporter molecule in live cells and may be a useful tool with far-reaching applicability for a variety of applications.
Allott, L., Chen, C., Braga, M., Leung, S. F. J., Wang, N., Barnes, C., …Aboagye, E. O. (in press). Detecting hypoxia in vitro using 18F-pretargeted IEDDA “click” chemistry in live cells. RSC advances, 11(33), 20335-20341. https://doi.org/10.1039/d1ra02482e
Journal Article Type | Article |
---|---|
Acceptance Date | Jun 1, 2021 |
Online Publication Date | Jun 7, 2021 |
Deposit Date | Jun 7, 2021 |
Publicly Available Date | Oct 27, 2022 |
Journal | RSC Advances |
Print ISSN | 2046-2069 |
Publisher | Royal Society of Chemistry |
Peer Reviewed | Peer Reviewed |
Volume | 11 |
Issue | 33 |
Pages | 20335-20341 |
DOI | https://doi.org/10.1039/d1ra02482e |
Keywords | General Chemistry; General Chemical Engineering |
Public URL | https://hull-repository.worktribe.com/output/3786690 |
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© 2021 The Author(s). Published by the Royal Society of Chemistry. Creative Commons Licence: Attribution License. See: http://creativecommons.org/licenses/by/3.0/
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