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Controlling Intracellular Macrocyclization for the Imaging of Protease Activity


  • This research was supported by the Stanford University National Cancer Institute (NCI) Centers of Cancer Nanotechnology Excellence (1U54A151459-01), the NCI ICMIC@Stanford (1P50A114747-06), and an IDEA award from the Department of Defense Breast Cancer Research Program (W81XWH-09-1-0057).


original image

Reporters on the ground: An intramolecular macrocyclization reaction took place highly efficiently in live cells under the control of a specific enzyme and reduction by glutathione (GSH; see picture). Macrocyclic products (represented as blue rings) synthesized in cells self-assembled into nanoparticles aggregated and retained at the site near the enzyme location to report local proteolytic activity in live cells.