Bioluminescent-based imaging and quantification of glucose uptake in vivo

Glucose is a major source of energy for most living organisms and its aberrant uptake is linked to many pathological conditions. However, our understanding of disease-associated glucose flux is limited due to the lack of robust tools. To date, positron emission tomography (PET) imaging remains the gold standard for measuring glucose uptake, and no optical tools exist for non-invasive longitudinal imaging of this important metabolite in in vivo settings. Here we report the development of a novel bioluminescent glucose uptake probe (BiGluc) for real-time, non-invasive longitudinal imaging of glucose absorption both in vitro and in vivo. In addition, we demonstrate that the sensitivity of our method is comparable with commonly used (18)F-FDG-PET tracers and validate BiGluc as a tool for the identification of novel glucose transport inhibitors. The new imaging reagent enables a wide range of applications in the field of metabolism and drug development.