Inhibitory effect of diethyl pyrocarbonate on the H+/organic cation antiport system in rat renal brush-border membranes.
作者： R Hori , H Maegawa , M Kato , T Katsura , K Inui
DOI: 10.1016/S0021-9258(18)63846-3
关键词: Chemistry 、 Antiporter 、 Histidine 、 Medicinal chemistry 、 Ion transporter 、 Membrane transport 、 Chromatography 、 Organic anion 、 Tetraethylammonium 、 Renal cortex 、 Hydroxylamine
摘要: We examined the effect of diethyl pyrocarbonate (DEPC), a histidine-specific reagent, on H+/organic cation antiport system in brush-border membrane vesicles isolated from rat renal cortex. Pretreatment with DEPC resulted inhibition tetraethylammonium transport. This was reversed by subsequent treatment hydroxylamine, but not dithiotreitol. In contrast, uptake p-aminohippurate, typical organic anion, inhibited pretreatment. absence an H+ gradient, pretreatment at pH 6.0-7.0, 7.5. The Vmax value 7.0 decreased without any change Km value, kinetic parameters 7.5 were unchanged. Unlabeled tetraethylamonium did protect against DEPC. These results suggest that histidine residues carrier are essential for transport acidic and neutral values, alkaline play important role as regulatory sites rather than binding cations.
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