Identification and characterization of potent and selective aquaporin-3 and aquaporin-7 inhibitors.

ABSTRACT: The aquaglyceroporins are a subfamily of aquaporins that conduct both water and glycerol. Aquaporin-3 (AQP3) has an important physiological function in renal water reabsorption, and AQP3-mediated hydrogen peroxide (H₂O₂) permeability can enhance cytokine signaling in several cell types. The related aquaglyceroporin AQP7 is required for dendritic cell chemokine responses and antigen uptake. Selective small-molecule inhibitors are desirable tools for investigating the biological and pathological roles of these and other AQP isoforms. Here, using a calcein fluorescence quenching assay, we screened a library of 7360 drug-like small molecules for inhibition of mouse AQP3 water permeability. Hit confirmation and expansion with commercially available substances identified th

SUBMITTER: Sonntag Y 

PROVIDER: S-EPMC6509502 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature