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Statements

Subject Item
n2:RIV%2F00064165%3A_____%2F12%3A11398%21RIV13-MZ0-00064165
rdf:type
skos:Concept n16:Vysledek
rdfs:seeAlso
http://dx.doi.org/10.1016/j.bmc.2012.01.037
dcterms:description
Selective neuronal nitric oxide synthase (nNOS) inhibitors have therapeutic applications in the treatment of numerous neurodegenerative diseases. Here we report the synthesis and evaluation of a series of inhibitors designed to have increased cell membrane permeability via intramolecular hydrogen bonding. Their potencies were examined in both purified enzyme and cell-based assays; a comparison of these results demonstrates that two of the new inhibitors display significantly increased membrane permeability over previous analogs. NMR spectroscopy provides evidence of intramolecular hydrogen bonding under physiological conditions in two of the inhibitors. Crystal structures of the inhibitors in the nNOS active site confirm the predicted non-intramolecular hydrogen bonded binding mode. Intramolecular hydrogen bonding may be an effective approach for increasing cell membrane permeability without affecting target protein binding. (C) 2012 Elsevier Ltd. All rights reserved. Selective neuronal nitric oxide synthase (nNOS) inhibitors have therapeutic applications in the treatment of numerous neurodegenerative diseases. Here we report the synthesis and evaluation of a series of inhibitors designed to have increased cell membrane permeability via intramolecular hydrogen bonding. Their potencies were examined in both purified enzyme and cell-based assays; a comparison of these results demonstrates that two of the new inhibitors display significantly increased membrane permeability over previous analogs. NMR spectroscopy provides evidence of intramolecular hydrogen bonding under physiological conditions in two of the inhibitors. Crystal structures of the inhibitors in the nNOS active site confirm the predicted non-intramolecular hydrogen bonded binding mode. Intramolecular hydrogen bonding may be an effective approach for increasing cell membrane permeability without affecting target protein binding. (C) 2012 Elsevier Ltd. All rights reserved.
dcterms:title
Intramolecular hydrogen bonding: A potential strategy for more bioavailable inhibitors of neuronal nitric oxide synthase Intramolecular hydrogen bonding: A potential strategy for more bioavailable inhibitors of neuronal nitric oxide synthase
skos:prefLabel
Intramolecular hydrogen bonding: A potential strategy for more bioavailable inhibitors of neuronal nitric oxide synthase Intramolecular hydrogen bonding: A potential strategy for more bioavailable inhibitors of neuronal nitric oxide synthase
skos:notation
RIV/00064165:_____/12:11398!RIV13-MZ0-00064165
n16:predkladatel
n17:ico%3A00064165
n3:aktivita
n15:Z n15:I
n3:aktivity
I, Z(MSM0021620849)
n3:cisloPeriodika
7
n3:dodaniDat
n13:2013
n3:domaciTvurceVysledku
n18:4688678
n3:druhVysledku
n7:J
n3:duvernostUdaju
n12:S
n3:entitaPredkladatele
n5:predkladatel
n3:idSjednocenehoVysledku
142755
n3:idVysledku
RIV/00064165:_____/12:11398
n3:jazykVysledku
n19:eng
n3:klicovaSlova
Neuronal nitric oxide synthase; Enzyme inhibitors; Intramolecular hydrogen bond; escherichia-coli; monocationic inhibitors; selective inhibitors; drug discovery; cerebral-palsy; active-site; disease; model; analogs; design
n3:klicoveSlovo
n6:cerebral-palsy n6:model n6:monocationic%20inhibitors n6:active-site n6:Intramolecular%20hydrogen%20bond n6:escherichia-coli n6:disease n6:Enzyme%20inhibitors n6:Neuronal%20nitric%20oxide%20synthase n6:selective%20inhibitors n6:drug%20discovery n6:analogs n6:design
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[3CD84A7D5264]
n3:nazevZdroje
Bioorganic & Medicinal Chemistry
n3:obor
n11:CE
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
10
n3:rokUplatneniVysledku
n13:2012
n3:svazekPeriodika
20
n3:tvurceVysledku
Ji, H. T. Kraus, JM Poulos, TL Labby, KJ Martásek, Pavel Silverman, RB Mataka, J. Li, HY Roman, LJ Xue, FT
n3:wos
000301379300027
n3:zamer
n10:MSM0021620849
s:issn
0968-0896
s:numberOfPages
9