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Detecting hypoxia in vitro using 18F-pretargeted IEDDA “click” chemistry in live cells

Allott, Louis; Chen, Cen; Braga, Marta; Leung, Sau Fung Jacob; Wang, Ning; Barnes, Chris; Brickute, Diana; Carroll, Laurence; Aboagye, Eric O.

Authors

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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



Abstract

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.

Citation

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 Jun 8, 2021
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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