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Aquaporin-3 (AQP3) is a member of the aquaglyceroporin subfamily of water channels, uniquely capable of transporting both water and small uncharged solutes like glycerol and urea across cell membranes (UniProt P41181). It is predominantly expressed in the basal layer of the epidermis, where it plays a critical role in maintaining skin hydration, elasticity, and barrier function by regulating glycerol content (PubMed: 15869245). Beyond the skin, AQP3 is involved in cell proliferation and migration, making it a significant factor in wound healing and cancer progression, particularly in epithelial-derived tumors (PubMed: 23152193). In various cancers, AQP3 overexpression is linked to increased metastasis and metabolic reprogramming through enhanced glycerol uptake. Therapeutic targeting of AQP3 primarily focuses on small-molecule inhibitors, such as gold-based compounds, to treat skin disorders or inhibit tumor growth (PubMed: 21908561). However, the development of selective inhibitors remains a challenge due to the structural similarity among aquaporin isoforms.
Inhibition of the channel pore to block the transmembrane flux of water and glycerol.
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