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• W2201186768 abstract "Aquaporins ( AQP s) are a family of membrane proteins that function as channels facilitating water transport in response to osmotic gradients. These play critical roles in several normal physiological and pathological states and are targets for drug discovery. Selective inhibition of the AQP 1 water channel may provide a new approach for the treatment of several disorders including ocular hypertension/glaucoma, congestive heart failure, brain swelling associated with a stroke, corneal and macular edema, pulmonary edema, and otic disorders such as hearing loss and vertigo. We developed a high‐throughput assay to screen a library of compounds as potential AQP 1 modulators by monitoring the fluorescence dequenching of entrapped calcein in a confluent layer of AQP 1‐overexpressing CHO cells that were exposed to a hypotonic shock. Promising candidates were tested in a X enopus oocyte‐swelling assay, which confirmed the identification of two lead classes of compounds belonging to aromatic sulfonamides and dihydrobenzofurans with IC 50 s in the low micromolar range. These selected compounds directly inhibited water transport in AQP 1‐enriched stripped erythrocyte ghosts and in proteoliposomes reconstituted with purified AQP 1. Validation of these lead compounds, by the three independent assays, establishes a set of attractive AQP 1 blockers for developing novel, small‐molecule functional modulators of human AQP 1." @default.
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• W2201186768 date "2016-01-17" @default.
• W2201186768 modified "2023-09-26" @default.
• W2201186768 title "Rapid Identification of Novel Inhibitors of the Human Aquaporin‐1 Water Channel" @default.
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• W2201186768 doi "https://doi.org/10.1111/cbdd.12713" @default.
• W2201186768 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5065099" @default.
• W2201186768 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26685080" @default.
• W2201186768 hasPublicationYear "2016" @default.
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