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Issue 33, 2021

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

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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.

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

Supplementary files

Article information


Submitted
29 Mar 2021
Accepted
01 Jun 2021
First published
07 Jun 2021

This article is Open Access

RSC Adv., 2021,11, 20335-20341
Article type
Paper

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

L. Allott, C. Chen, M. Braga, S. F. J. Leung, N. Wang, C. Barnes, D. Brickute, L. Carroll and E. O. Aboagye, RSC Adv., 2021, 11, 20335 DOI: 10.1039/D1RA02482E

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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