Herein, we report a condensation system which could be controlled by furin, an important protease which is associated with early development of cancer. We designed Acetyl-Arg-Val-Arg-Arg-Cys(StBu)-Tyr(I-125)-CBT (1  ) for self-assembling radioactive nanoparticles (I125-NPs) in living cells. Its scrambled control Acetyl-Arg-Tyr(I-125)-Arg-Cys(StBu)-Arg-Val-CBT (1-scr  ) which can not be cleaved by furin was also prepared for study in parallel. At 160 min after cell efflux, 17.9% of the radioactivity was retained in the cells incubated with 1  and 100 �M 1-cold  while the percentages of other three groups are 4.4%, 3.7%, and 3.7% respectively. By means of intracellular assembly of radioactive nanoparticles, this provides us with a new method of furin detection or cancer early detection.Figure 1  . (a) Chemical structures of four compounds for this study. (b) Time course of cellular efflux of 1  and 1-scr  after the incubation with cells with/without co-incubation of 1-cold  or 1-scr-cold  at 100 �M for 30 min. (c) Radioactivity retained in cells after 160 minutes' efflux.

Furin controlled intracellular assembly of nanoparticles for enhanced uptake of radionuclide in living cells

243rd National Meeting (2012)

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