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Inhibitors of Mammalian Aquaporin Water Channels

School of Life & Health Sciences, Aston University, Aston Triangle, Birmingham B4 7ET, UK
Department of Cell Biology, Harvard Medical School, 200 Longwood Avenue, Boston, MA 02115, USA
Program in Cellular and Molecular Medicine, Boston Children’s Hospital, 200 Longwood Avenue, Boston, MA 02115, USA
Research Institute of Health Sciences, School of Sciences, University of Wolverhampton, Wolverhampton WV1 1LY, UK
Institute of Clinical Sciences, College of Medical and Dental Sciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, UK
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(7), 1589;
Received: 28 February 2019 / Revised: 25 March 2019 / Accepted: 26 March 2019 / Published: 29 March 2019
(This article belongs to the Special Issue Aquaporins: Water Channels Essential for Living Organisms 2.0)
Aquaporins (AQPs) are water channel proteins that are essential to life, being expressed in all kingdoms. In humans, there are 13 AQPs, at least one of which is found in every organ system. The structural biology of the AQP family is well-established and many functions for AQPs have been reported in health and disease. AQP expression is linked to numerous pathologies including tumor metastasis, fluid dysregulation, and traumatic injury. The targeted modulation of AQPs therefore presents an opportunity to develop novel treatments for diverse conditions. Various techniques such as video microscopy, light scattering and fluorescence quenching have been used to test putative AQP inhibitors in both AQP-expressing mammalian cells and heterologous expression systems. The inherent variability within these methods has caused discrepancy and many molecules that are inhibitory in one experimental system (such as tetraethylammonium, acetazolamide, and anti-epileptic drugs) have no activity in others. Some heavy metal ions (that would not be suitable for therapeutic use) and the compound, TGN-020, have been shown to inhibit some AQPs. Clinical trials for neuromyelitis optica treatments using anti-AQP4 IgG are in progress. However, these antibodies have no effect on water transport. More research to standardize high-throughput assays is required to identify AQP modulators for which there is an urgent and unmet clinical need. View Full-Text
Keywords: aquaporin; AQP inhibitors; AQP modulators; functional assays; AQP expression; AQPs in disease; AQP structure; TGN-020; heavy metals; small molecule inhibitors aquaporin; AQP inhibitors; AQP modulators; functional assays; AQP expression; AQPs in disease; AQP structure; TGN-020; heavy metals; small molecule inhibitors
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MDPI and ACS Style

Abir-Awan, M.; Kitchen, P.; Salman, M.M.; Conner, M.T.; Conner, A.C.; Bill, R.M. Inhibitors of Mammalian Aquaporin Water Channels. Int. J. Mol. Sci. 2019, 20, 1589.

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