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Exploiting in vitro and in vivo bioluminescence for the implementation of the three Rs principle (replacement, reduction, and refinement) in drug discovery

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Abstract

Bioluminescence-based analytical tools are suitable for high-throughput and high-content screening assays, finding widespread application in several fields related to the drug discovery process. Cell-based bioluminescence assays, because of their peculiar advantages of predictability, possibility of automation, multiplexing, and miniaturization, seem the most appealing tool for the high demands of the early stages of drug screening. Reporter gene technology and the bioluminescence resonance energy transfer principle are widely used, and receptor binding studies of new agonists/antagonists for a variety of human receptors expressed in different cell lines can be performed. Moreover, bioluminescence can be used for in vitro and in vivo real-time monitoring of pathophysiological processes within living cells and small animals. New luciferases and substrates have recently arrived on the market, further expanding the spectrum of applications. A new generation of probes are also emerging that promise to revolutionize the preclinical imaging market. This formidable toolbox is demonstrated to facilitate the implementation of the three Rs principle in the early drug discovery process, in compliance with ethical and responsible research to reduce cost and improve the reliability and predictability of results.

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Authors and Affiliations

  1. Department of Chemistry “G. Ciamician, University of Bologna, Via Selmi 2, 40126, Bologna, Italy

    Elisa Michelini, Donato Calabria & Aldo Roda

  2. Istituto Nazionale di Biostrutture e Biosistemi, 00136, Rome, Italy

    Elisa Michelini, Luca Cevenini, Maria Maddalena Calabretta & Aldo Roda

  3. Health Sciences and Technologies Interdepartmental Center for Industrial Research, University of Bologna, 40126, Bologna, Italy

    Donato Calabria

Authors
  1. Elisa Michelini
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  2. Luca Cevenini
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  3. Maria Maddalena Calabretta
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  4. Donato Calabria
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  5. Aldo Roda
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Correspondence to Elisa Michelini.

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Published in the topical collection Analytical Bioluminescence and Chemiluminescence with guest editors Elisa Michelini and Mara Mirasoli.

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Michelini, E., Cevenini, L., Calabretta, M.M. et al. Exploiting in vitro and in vivo bioluminescence for the implementation of the three Rs principle (replacement, reduction, and refinement) in drug discovery. Anal Bioanal Chem 406, 5531–5539 (2014). https://doi.org/10.1007/s00216-014-7925-2

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  • DOI: https://doi.org/10.1007/s00216-014-7925-2

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