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Issue 48, 2017
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Prolonged bioluminescence imaging in living cells and mice using novel pro-substrates for Renilla luciferase

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Abstract

The prodrug or caged-luciferin strategy affords an excellent platform for persistent bioluminescence imaging. In the current work, we designed and synthesized ten novel pro-substrates for Renilla luciferase by introducing ester protecting groups of different sizes into the carbonyl group of the free luciferin 1. Taking advantage of intracellular esterases, lipases, and nucleophilic substances, the ester protecting groups were hydrolyzed, resulting in the release of a free luciferin and a bioluminescence signal turn-on. Among the tested pro-substrates, the butyryloxymethyl luciferin 7 exhibited low cytotoxicity and a prolonged luminescence signal both in cellulo and in vivo. Therefore, the butyryloxymethyl luciferin 7 can act as a promising substrate for noninvasive extended imaging in diagnostic and therapeutic fields.

Graphical abstract: Prolonged bioluminescence imaging in living cells and mice using novel pro-substrates for Renilla luciferase

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Publication details

The article was received on 06 Jul 2017, accepted on 16 Nov 2017 and first published on 16 Nov 2017


Article type: Paper
DOI: 10.1039/C7OB01656E
Citation: Org. Biomol. Chem., 2017,15, 10238-10244
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    Prolonged bioluminescence imaging in living cells and mice using novel pro-substrates for Renilla luciferase

    M. Yuan, X. Ma, T. Jiang, Y. Gao, Y. Cui, C. Zhang, X. Yang, Y. Huang, L. Du, I. Yampolsky and M. Li, Org. Biomol. Chem., 2017, 15, 10238
    DOI: 10.1039/C7OB01656E

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