Exploring the gating mechanisms of aquaporin-3: new clues for the design of inhibitors?

A. de Almeida; A. P. Martins; A. F. Mósca; H. J. Wijma; C. Prista; G. Soveral; A. Casini

doi:10.1039/C6MB00013D

Exploring the gating mechanisms of aquaporin-3: new clues for the design of inhibitors?†

A. de Almeida,‡^a A. P. Martins,‡^bc A. F. Mósca,^bc H. J. Wijma,^d C. Prista,^e G. Soveral*^bc and A. Casini*^af

* Corresponding authors

^a Dept. of Pharmacokinetics, Toxicology and Targeting, Groningen Research Institute of Pharmacy, University of Groningen, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands

^b Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal
E-mail: gsoveral@ff.ulisboa.pt

^c Dept. Bioquímica e Biologia Humana, Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal

^d Department of Biochemistry, Groningen Biomolecular Sciences and Biotechnology Institute, University of Groningen, Nijenborgh 4, 9747 AG Groningen, The Netherlands

^e Research Center “Linking Landscape, Environment, Agriculture and Food” (LEAF), Instituto Superior de Agronomia, Universidade de Lisboa, 1349-017 Lisboa, Portugal

^f School of Chemistry, Cardiff University, Main Building, Park Place, Cardiff CF10 3AT, UK
E-mail: casinia@cardiff.ac.uk

Abstract

The pH gating of human AQP3 and its effects on both water and glycerol permeabilities have been fully characterized for the first time using a human red blood cell model (hRBC). For comparison, the effects of pH on the gating of rat AQP3 have also been characterized in yeast. The obtained results highlight similarities as well as differences between the two isoforms. In addition, we investigated the molecular mechanism of hAQP3 pH gating in silico, which may disclose new pathways to AQP regulation by small molecule inhibitors, and therefore may be important for drug development.

This article is part of the themed collection: Chemical Biology in Molecular BioSystems

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DOI: https://doi.org/10.1039/C6MB00013D
Article type: Paper
Submitted: 06 ጃንዩ 2016
Accepted: 02 ማርች 2016
First published: 02 ማርች 2016

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Mol. BioSyst., 2016,12, 1564-1573

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Exploring the gating mechanisms of aquaporin-3: new clues for the design of inhibitors?

A. de Almeida, A. P. Martins, A. F. Mósca, H. J. Wijma, C. Prista, G. Soveral and A. Casini, Mol. BioSyst., 2016, 12, 1564 DOI: 10.1039/C6MB00013D

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Molecular BioSystems

Exploring the gating mechanisms of aquaporin-3: new clues for the design of inhibitors?†

Abstract

Supplementary files

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Exploring the gating mechanisms of aquaporin-3: new clues for the design of inhibitors?

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