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Issue 78, 2015
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Discovery of a series of 2-phenylnaphthalenes as firefly luciferase inhibitors

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Abstract

As the most convenient and efficient bioluminescence system, the firefly luciferase/luciferin complex has been widely used in life science research and high-throughput screening (HTS). Nonetheless, the interpretation of firefly luciferase-based assay data is often complicated by the occurrence of “false positives,” in part because firefly luciferase (Fluc) is subject to direct inhibition by HTS compounds that might inadvertently act as inhibitors of its catalytic site. Here we report a series of 2-phenylnaphthalenes as Fluc inhibitors with suitable potency both in vitro and in vivo. Besides, our compound 5 showed significant systemic inhibition in transgenic mice. Enzymatic kinetics study reveals that compound 5 is competitive for substrate aminoluciferin and noncompetitive for the second substrate ATP. Furthermore, compound 5 exhibited good performance as a quenching agent in a dual-luciferase reporter assay. We anticipate that these Fluc inhibitors will contribute to the broader utilization of bioluminescence in life science research while circumventing or at least reducing the number of “false positives”.

Graphical abstract: Discovery of a series of 2-phenylnaphthalenes as firefly luciferase inhibitors

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Publication details

The article was received on 02 Jul 2015, accepted on 08 Jul 2015 and first published on 08 Jul 2015


Article type: Paper
DOI: 10.1039/C5RA12886B
Author version available: Download Author version (PDF)
Citation: RSC Adv., 2015,5, 63450-63457
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    Discovery of a series of 2-phenylnaphthalenes as firefly luciferase inhibitors

    H. Bai, W. Chen, W. Wu, Z. Ma, H. Zhang, T. Jiang, T. Zhang, Y. Zhou, L. Du, Y. Shen and M. Li, RSC Adv., 2015, 5, 63450
    DOI: 10.1039/C5RA12886B

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