A boronate-caged [18F]FLT probe for hydrogen peroxide detection using positron emission tomography Journal Article


Authors: Carroll, V.; Michel, B. W.; Blecha, J.; Vanbrocklin, H.; Keshari, K.; Wilson, D.; Chang, C. J.
Article Title: A boronate-caged [18F]FLT probe for hydrogen peroxide detection using positron emission tomography
Abstract: Reactive oxygen species (ROS) play important roles in the development and progression of cancer and other diseases, motivating the development of translatable technologies for biological ROS imaging. Here we report Peroxy-Caged-[18F]Fluorodeoxy thymidine-1 (PC-FLT-1), an oxidatively immolative positron emission tomography (PET) probe for H2O2 detection. PC-FLT-1 reacts with H2O2 to generate [18F]FLT, allowing its peroxide-dependent uptake and retention in proliferating cells. The relative uptake of PC-FLT-1 was evaluated using H2O2-treated UOK262 renal carcinoma cells and a paraquat-induced oxidative stress cell model, demonstrating ROS-dependent tracer accumulation. The data suggest that PC-FLT-1 possesses promising characteristics for translatable ROS detection and provide a general approach to PET imaging that can be expanded to the in vivo study of other biologically relevant analytes.
Keywords: unclassified drug; positron emission tomography; cell proliferation; in vivo study; kidney carcinoma; cancer cell; reactive oxygen metabolite; hydrogen peroxide; oxidative stress; boronic acid derivative; thymidine derivative; article; boronate; hydrogen peroxide detections; fluorodeoxy thymidine 1 f 18; paraquat
Journal Title: Journal of the American Chemical Society
Volume: 136
Issue: 42
ISSN: 0002-7863
Publisher: American Chemical Society  
Date Published: 2014-10-22
Start Page: 14742
End Page: 14745
Language: English
DOI: 10.1021/ja509198w
PROVIDER: scopus
PMCID: PMC4210116
PUBMED: 25310369
DOI/URL:
Notes: Export Date: 1 December 2014 -- Source: Scopus
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