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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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Article information


Submitted
20 Jun 2014
Accepted
20 Jul 2014
First published
22 Jul 2014

Med. Chem. Commun., 2014,5, 1444-1453
Article type
Review Article
Author version available

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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