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@ARTICLE{Minozzi:201194,
author = {Minozzi, Manuela and Lattanzi, Gianluca and Benz, Roland
and Costi, Maria P. and Venturelli, Alberto and Carloni,
Paolo},
title = {{P}ermeation through the {C}ell {M}embrane of a
{B}oron-{B}ased β-{L}actamase {I}nhibitor},
journal = {PLoS one},
volume = {6},
number = {8},
issn = {1932-6203},
address = {Lawrence, Kan.},
publisher = {PLoS},
reportid = {FZJ-2015-03499},
pages = {e23187 -},
year = {2011},
abstract = {Bacteria express beta-lactamases to counteract the
beneficial action of antibiotics.
Benzo[b]-thiophene-2-boronic acid (BZB) derivatives are
β-lactamase inhibitors and, as such, promising compounds to
be associated with β-lactam antibacterial therapies. The
uncharged form of BZB, in particular, is suggested to
diffuse through the outer membrane of Gram negative
bacteria. In this study, through the combination of
electrophysiological experiments across reconstituted
PC/n-decane bilayers and metadynamics-based free energy
calculations, we investigate the permeation mechanism of
boronic compounds. Our experimental data establish that BZB
passes through the membrane, while computer simulations
provide hints for the existence of an aqueous, water-filled
monomolecular channel. These findings provide new
perspectives for the design of boronic acid derivatives with
high membrane permeability.},
cin = {GRS / IAS-5},
ddc = {500},
cid = {I:(DE-Juel1)GRS-20100316 / I:(DE-Juel1)IAS-5-20120330},
pnm = {899 - ohne Topic (POF2-899)},
pid = {G:(DE-HGF)POF2-899},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000294121300018},
doi = {10.1371/journal.pone.0023187},
url = {https://juser.fz-juelich.de/record/201194},
}