PMID:15642346

Citation	Dibrov, P, Rimon, A, Dzioba, J, Winogrodzki, A, Shalitin, Y and Padan, E (2005) 2-Aminoperimidine, a specific inhibitor of bacterial NhaA Na(+)/H(+) antiporters. FEBS Lett. 579:373-8
Abstract	The diuretic drug amiloride and its numerous derivatives are competitive inhibitors of mammalian Na(+)/H(+) antiporters and other eukaryotic antiporters. Most prokaryotic antiporters, including the major NhaA family of enterobacteria, are resistant to these compounds. We show that 2-aminoperimidine (AP), a guanidine-containing naphthalene derivative with some similarity to amiloride, acts as a specific inhibitor of NhaA from Escherichia coli. Similar concentrations (IC(50) of 0.9 muM) inhibit the proton motive force dependent Na(+)(Li(+))/H(+) exchange reaction in inside-out sub-bacterial vesicles (at 10 mM NaCl, pH 8) as well as the initial rate of (22)Na(+)/Na(+) exchange mediated by pure NhaA in proteoliposomes. The inhibitor is specific to NhaA type antiporters, so AP is a new tool to study the mechanism and roles of NhaA antiporters of enterobacteria as well as the molecular basis of inhibition by an amiloride-like compound.
Links	PubMed Online version:10.1016/j.febslet.2004.11.098
Keywords	Amiloride/analogs & derivatives; Cell Membrane/physiology; Escherichia coli Proteins/antagonists & inhibitors; Proteolipids/drug effects; Proteolipids/physiology; Quinazolines/chemistry; Quinazolines/pharmacology; Sodium/metabolism; Sodium-Hydrogen Antiporter/antagonists & inhibitors
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