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Updated: Nov 1, 2025
Detection of Microregional Hypoxia in Mouse Cerebral Cortex by Two-photon Imaging of Endogenous NADH Fluorescence
Published on: February 21, 2012
Detecting hypoxia in vitro using 18F-pretargeted IEDDA "click" chemistry in live cells
Louis Allott1,2, Cen Chen1, Marta Braga1
1Comprehensive Cancer Imaging Centre, Faculty of Medicine, Department of Surgery and Cancer, Imperial College London, Hammersmith Hospital Du Cane Road London W12 0NN UK eric.aboagye@imperial.ac.uk.
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.
