Abstract
Aquaporins (AQP) working as membrane channels facilitated water transport, play vital roles in various physiological progress including cell migration, energy metabolism, inflammation, etc. They are quite important drug targets, but elusive for discovery due to their undruggable properties. In this chapter, we summarized most fluently used methods for screening AQP inhibitors, including cell swelling assay, cell shrinking assay, and stopped-flow assay. And three classes of AQP inhibitors have been discussed, including metal-related inhibitors, quaternary ammonium salts, and small molecule inhibitors which further divided into four parts, sulfanilamide analogies, TGN-020, antiepileptic drugs, and others. It has been suggested that although they showed inhibition effects on AQP1, AQP3, AQP4, AQP7, or AQP9 in some researches, none of them could be asserted as AQP inhibitors to some extent. Discovering AQP inhibitors is a big challenge, but if successful, it will be a great contribution for human health.
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