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Issue Date
2019-03-29
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Show full item recordAbstract
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.Citation
Abir-Awan, M., Kitchen, P., Salman, M. M., Conner, M. T., Conner, A. C., & Bill, R. M. (2019) Inhibitors of Mammalian Aquaporin water Channels. International Journal of Molecular Sciences, 20(7), p. 1589. https://doi.org/10.3390/ijms20071589Publisher
MDPI AGJournal
International journal of molecular sciencesPubMed ID
30934923Additional Links
https://www.mdpi.com/1422-0067/20/7/1589Type
Journal articleLanguage
enEISSN
1422-0067ae974a485f413a2113503eed53cd6c53
10.3390/ijms20071589
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Except where otherwise noted, this item's license is described as Licence for published version: Creative Commons Attribution 4.0 International
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