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Type: Journal article
Title: Recent breakthroughs and future directions in drugging aquaporins
Author: Salman, M.M.
Kitchen, P.
Yool, A.J.
Bill, R.M.
Citation: Trends in Pharmacological Sciences, 2022; 43(1):30-42
Publisher: Elsevier
Issue Date: 2022
ISSN: 0165-6147
Statement of
Mootaz M. Salman, Philip Kitchen, Andrea J. Yool and Roslyn M. Bill
Abstract: Aquaporins facilitate the passive transport of water, solutes, or ions across biological membranes. They are implicated in diverse pathologies including brain edema following stroke or trauma, epilepsy, cancer cell migration and tumor angiogenesis, metabolic disorders, and inflammation. Despite this, there is no aquaporin-targeted drug in the clinic and aquaporins have been perceived to be intrinsically non-druggable targets. Here we challenge this idea, as viable routes to inhibition of aquaporin function have recently been identified, including targeting their regulation or their roles as channels for unexpected substrates. Identifying new drug development frameworks for conditions associated with disrupted water and solute homeostasis will meet the urgent, unmet clinical need of millions of patients for whom no pharmacological interventions are available.
Keywords: Aquaporins; subcellular localization; trafficking; ion channels; edema; fluid transport; osmosis
Rights: © 2021 The Author(s). Published by Elsevier Ltd. This is an open access article under the CC BY license (
DOI: 10.1016/
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Appears in Collections:Pharmacology publications

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