Design, synthesis and assaying of potential aquaporin inhibitors.
The aquaporin protein family performs fundamental tasks in the physiology of several organs in the human body. Their roles in several disorders known to involve water movement make them attractive targets for the development of novel drug therapies.This chapter describes assays commonly used to study the water permeability across AQPs. It also describes the effect of some known inhibitors of aquaporins on water permeability, such as mercury, gold, silver, copper, phloretin, tetraethyl ammonium salts and acetazolamide compounds.
Haddoub
Rose
R
Manchester Interdisciplinary Biocentre (MIB) & The School of Chemistry, University of Manchester, 131 Princess Street, Manchester, M1 7DN, UK.
Rützler
Michael
M
Robin
Aélig
A
Flitsch
Sabine L
SL
D000818:Animals; D020346:Aquaporins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D001681:Biological Assay / Q000379:methods; D002463:Cell Membrane Permeability / Q000187:drug effects*; D015195:Drug Design; D005456:Fluorescent Dyes; D006801:Humans; D007201:Indicator Dilution Techniques; D008670:Metals / Q000494:pharmacology; D015394:Molecular Structure; D010693:Phloretin / Q000494:pharmacology; D011487:Protein Conformation; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology; D014867:Water / Q000378:metabolism*
D020346:Aquaporins; D005456:Fluorescent Dyes; D008670:Metals; D000644:Quaternary Ammonium Compounds; D013449:Sulfonamides; D014867:Water; D010693:Phloretin