A gold coordination compound as a chemical probe to unravel aquaporin-7 function

Madeira, Ana, De Almeida, Andreia ORCID: https://orcid.org/0000-0002-6889-1503, de Graaf, Chris, Camps, Marta, Zorzano, Antonio, Moura, Teresa F., Casini, Angela ORCID: https://orcid.org/0000-0003-1599-9542 and Soveral, Graca 2014. A gold coordination compound as a chemical probe to unravel aquaporin-7 function. ChemBioChem 15 (10) , pp. 1487-1494. 10.1002/cbic.201402103

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Abstract

Aquaporins (AQPs) are membrane water/glycerol channels that are involved in many physiological functions. Aquaporin-based modulators are predicted to have potential utility in the treatment of several diseases, as well as chemical tools to assess AQPs function in biological systems. We recently reported gold(III) compounds as human AQP3 inhibitors, with Auphen as the most potent of the series. In this work, we assessed the modulation of aquaporin-7 (AQP7) expressed in an adipocyte cell model and show that Auphen significantly inhibits mouse and human AQP7. By homology modeling and molecular docking it was possible to identify the thioether groups of methionine residues, in particular Met47, as likely candidates for binding to the gold(III) complex. Our data point to Auphen as a useful chemical tool to detect AQP7 function. It might constitute a basis to develop inhibitors with improved affinity towards different aquaglyceroporin isoforms.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Chemistry
Subjects:	Q Science > QD Chemistry
Publisher:	Wiley-Blackwell
ISSN:	1439-4227
Last Modified:	31 Oct 2022 08:57
URI:	https://orca.cardiff.ac.uk/id/eprint/79303

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