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Overview
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Background
Thonzonium Bromide is a surface active agent and an inhibitor of V-ATPase proton transport with EC50 value of 69 µM [1] [2].
Vacuolar ATPases (V-ATPases) are proton pumps that maintain pH homeostasis. V-ATPases couple the energy of ATP hydrolysis to proton transport across intracellular membranes [2].
Thonzonium Bromide is a surface active agent and an inhibitor of V-ATPase proton transport. In wild-type yeast cells, thonzonium bromide significantly decreased the cytosolic pH to 6.22. In vacuolar membrane vesicles, thonzonium bromide inhibited proton transport with EC50 value of 69 µM in a dose-dependent way. However, thonzonium bromide didn’t inhibit ATP hydrolysis, which suggested that thonzonium bromide uncoupled V-ATPase proton pumps. In wild-type yeast cells, thonzonium bromide (1 µM) didn’t inhibit cell growth. However, thonzonium bromide inhibited cell growth at 10 µM and caused a mild vma (vacuolar membrane ATPase) mutant growth phenotype. At concentrations up to 50 and 100 µM, thonzonium bromide completely inhibited yeast growth [2].[1]. Chafetz L, Greenough RC, Frank J. Thermal decomposition of thonzonium bromide. Pharm Res, 1986, 3(5): 298-301.
[2]. Chan CY, Prudom C, Raines SM, et al. Inhibitors of V-ATPase proton transport reveal uncoupling functions of tether linking cytosolic and membrane domains of V0 subunit a (Vph1p). J Biol Chem, 2012, 287(13): 10236-10250.
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- Properties
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Overview