Search results for "Aquaporin"

showing 2 items of 42 documents

Mechanisms of irreversible aquaporin-10 inhibition by organogold compounds studied by combined biophysical methods and atomistic simulations

2021

Abstract The inhibition of glycerol permeation via human aquaporin-10 (hAQP10) by organometallic gold complexes has been studied by stopped-flow fluorescence spectroscopy, and its mechanism has been described using molecular modelling and atomistic simulations. The most effective hAQP10 inhibitors are cyclometalated Au(III) C^N compounds known to efficiently react with cysteine residues leading to the formation of irreversible C–S bonds. Functional assays also demonstrate the irreversibility of the binding to hAQP10 by the organometallic complexes. The obtained computational results by metadynamics show that the local arylation of Cys209 in hAQP10 by one of the gold inhibitors is mapped int…

waterBiophysicsGlycerol transportirreversible inhibitorsMolecular Dynamics SimulationAquaporinsBiochemistryBiophysical PhenomenaFluorescence spectroscopymetadynamicsBiomaterialsMolecular dynamicsGold CompoundsComputational chemistrygold compoundsHumansOrganogold CompoundsChemistryglycerol transportMetals and AlloysMetadynamicsPermeationSmall moleculeSpectrometry FluorescenceChemistry (miscellaneous)aquaglyceroporinOrganogold Compounds
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The AQP2 mutation V71M causesnephrogenic diabetes insipidus in humans but does not impair the function of a bacterial homolog

2015

Graphical abstract

wt wild-typeGpA glycophorin AHM half-membrane-spanningurogenital systemQH301-705.5AquaporinNephrogenic diabetes insipidusAQP ER endoplasmic reticulumGlpF glycerol facilitatorActivityProtein oligomerizationResearch articleNDI nephrogenic diabetes insipidusAVP arginine vasopressinGlpF500 Natural sciences and mathematicsAQP aquaporin500 NaturwissenschaftenBiology (General)AVPR2 V2 receptorComputingMethodologies_COMPUTERGRAPHICSTM transmembraneFEBS Open Bio
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