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2‐Aminoperimidine, a specific inhibitor of bacterial NhaA Na + /H + antiporters
Author(s) -
Dibrov Pavel,
Rimon Abraham,
Dzioba Judith,
Winogrodzki Arthur,
Shalitin Yechiel,
Padan Etana
Publication year - 2005
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2004.11.098
Subject(s) - antiporters , amiloride , chemistry , escherichia coli , biochemistry , sodium , antiporter , membrane , organic chemistry , gene
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 μM) 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.