Detecting hypoxia in vitro using 18F-pretargeted IEDDA “click” chemistry in live cells
File(s)
Published version
Author(s)
Type
Journal Article
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.
Date Issued
2021-06-07
Date Acceptance
2021-06-01
Citation
RSC Advances: an international journal to further the chemical sciences, 2021, 11 (33), pp.20335-20341
ISSN
2046-2069
Publisher
Royal Society of Chemistry
Start Page
20335
End Page
20341
Journal / Book Title
RSC Advances: an international journal to further the chemical sciences
Volume
11
Issue
33
Copyright Statement
© 2021 The Author(s). Published by the Royal Society of Chemistry. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
License URL
Sponsor
Medical Research Council
Identifier
https://pubs.rsc.org/en/content/articlelanding/2021/RA/D1RA02482E#!divAbstract
Subjects
03 Chemical Sciences
Publication Status
Published
Date Publish Online
2021-06-07