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Issue 10, 2014
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Gold compounds as aquaporin inhibitors: new opportunities for therapy and imaging

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Abstract

In recent years, gold-based compounds have been proved to hold promise in chemical biology being able to selectively inhibit proteins activities in cells and, therefore, to be exploited as either therapeutic agents or as chemical tools to detect protein/enzyme functions in living systems. In this area, we have recently described the properties of gold coordination complexes as potent and selective inhibitors of human aquaporins, protein channels involved in the transport of water and glycerol across biomembranes. Thus, we provide here an overview of the importance of aquaporins in various diseases and a detailed description of the state-of-the art progresses in the discovery of new inhibitors, including gold(III) complexes, and a description of their possible applications. Overall, the potential of coordination chemistry in providing compounds to modulate the activity of “elusive” drug targets, such as the aquaporins, will be discussed.

Graphical abstract: Gold compounds as aquaporin inhibitors: new opportunities for therapy and imaging

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Publication details

The article was received on 20 Jun 2014, accepted on 20 Jul 2014 and first published on 22 Jul 2014


Article type: Review Article
DOI: 10.1039/C4MD00265B
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Med. Chem. Commun., 2014,5, 1444-1453

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    Gold compounds as aquaporin inhibitors: new opportunities for therapy and imaging

    A. de Almeida, G. Soveral and A. Casini, Med. Chem. Commun., 2014, 5, 1444
    DOI: 10.1039/C4MD00265B

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