In vivo bioluminescence imaging of furin activity in breast cancer cells using bioluminogenic substrates.

ABSTRACT: Furin, a proprotein convertases family endoprotease, processes numerous physiological substrates and is overexpressed in cancer and inflammatory conditions. Noninvasive imaging of furin activity will offer a valuable tool to probe furin function over the course of tumor growth and migration in the same animals in real time and directly assess the inhibition efficacy of drugs in vivo. Here, we report successful bioluminescence imaging of furin activity in xenografted MBA-MB-468 breast cancer tumors in mice with bioluminogenic probes. The probes are conjugates of furin substrate, a consensus amino acid motif R-X-K/R-R (X, any amino acid), with the firefly luciferase substrate D-aminoluciferin. In the presence of the luciferase reporter, the probes are unable to produce bioluminescent emissio

SUBMITTER: Dragulescu-Andrasi A 

PROVIDER: S-EPMC2888877 | biostudies-literature | 2009 Aug

REPOSITORIES: biostudies-literature