caa a22 4500 467951837 CHVBK 20180405193743.0 cr unu---uuuuu 170328e20050101xx s 000 0 eng 10.1007/PL00021750 doi (NATIONALLICENCE)springer-10.1007/PL00021750 (NATIONALLICENCE)springer-10.1007/s10541-005-0048-9 Structure and activity of NO synthase inhibitors specific to the L-arginine binding site [Elektronische Daten] [S. Proskuryakov, A. Konoplyannikov, V. Skvortsov, A. Mandrugin, V. Fedoseev] Synthesis of compounds containing a fragment similar to the guanidine group of L-arginine, which is a substrate of nitric oxide synthase (NOS), is the main direction in creating NOS inhibitors. The inhibitory effect of such compounds is caused not only by their competition with the substrate for the L-arginine-binding site and/or oxidizing center of the enzyme (heme) but also by interaction with peptide motifs of the enzyme that influence its dimerization, affinity for cofactors, and interaction with associated proteins. Structures, activities, and relative in vitro and in vitro specificities of various NOS inhibitors (amino acid and non-amino acid) with linear or cyclic structure and containing guanidine, amidine, or isothiuronium group are considered. These properties are mainly analyzed by comparison with effects of the inhibitors on the inducible NOS. MAIK "Nauka/Interperiodica”, 2005 O2- : superoxide anion radical nationallicence BH4 : (6R)5,6,7,8-tetrahydro-L-biopterin nationallicence 1400W : N[3-(aminomethyl)-benzyl]-acetamidine nationallicence L-NA : Nωnitro-L-arginine nationallicence nitric oxide synthase (NOS) nationallicence NOS activity regulation nationallicence reactive oxygen species nationallicence substrate-like inhibitors nationallicence chemical structure nationallicence activity and selectivity of NOS inhibitors nationallicence NO⋅ : nitric oxide nationallicence ROS : reactive oxygen species nationallicence LPS : lipopolysaccharide nationallicence NOS : nitric oxide synthase nationallicence nNOS : neuronal NOS nationallicence iNOS : inducible NOS nationallicence eNOS : endothelial NOS nationallicence m-, r-, b-, and h-NOS : mouse, rat, bovine, and human NOS nationallicence CaM : calmodulin nationallicence ITU : isothiourea nationallicence AG : aminoguanidine nationallicence 2-AP : 2-aminopicoline nationallicence 7-NI : 7-nitroindazole nationallicence L-NMMA : Nω-monomethyl-L-arginine nationallicence PA : Nω-propyl-L-arginine nationallicence cPA : Nω-cyclopropyl-L-arginine nationallicence L-NIO : N5-iminoethyl-L-ornithine nationallicence L-VNIO : L-N5-(1-iminobuten-3-yl)-L-ornithine nationallicence L-NIL : N6-iminoethyl-L-lysine nationallicence L-TC : L-thiocitrulline nationallicence S-methyl-TC : S-methyl-L-thiocitrulline nationallicence 2-ADT : 2-amino-5,6-dihydro-4H-1,3-thiazine nationallicence $$\mathop O\nolimits_2^{\mathop .\limits^\_ }$$ : superoxide anion radical nationallicence 1400W : N-[3-(aminomethyl)-benzyl]-acetamidine nationallicence L-NA : Nω-nitro-L-arginine nationallicence BH4 : (6R)-5,6,7,8-tetrahydro-L-biopterin nationallicence Proskuryakov S. Medical Radiological Research Center, Russian Academy of Medical Sciences, ul. Koroleva 4, 249036, Obninsk, Russia aut Konoplyannikov A. Medical Radiological Research Center, Russian Academy of Medical Sciences, ul. Koroleva 4, 249036, Obninsk, Russia aut Skvortsov V. Medical Radiological Research Center, Russian Academy of Medical Sciences, ul. Koroleva 4, 249036, Obninsk, Russia aut Mandrugin A. Faculty of Chemistry, Lomonosov Moscow State University, 119992, Moscow, Russia aut Fedoseev V. Faculty of Chemistry, Lomonosov Moscow State University, 119992, Moscow, Russia aut Biochemistry (Moscow) Nauka/Interperiodica 70/1(2005-01-01), 8-23 0006-2979 70:1<8 2005 70 10541 https://doi.org/10.1007/PL00021750 text/html Onlinezugriff via DOI 1 review-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/PL00021750 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Proskuryakov S. Medical Radiological Research Center, Russian Academy of Medical Sciences, ul. Koroleva 4, 249036, Obninsk, Russia aut NATIONALLICENCE 700 1- Konoplyannikov A. Medical Radiological Research Center, Russian Academy of Medical Sciences, ul. Koroleva 4, 249036, Obninsk, Russia aut NATIONALLICENCE 700 1- Skvortsov V. Medical Radiological Research Center, Russian Academy of Medical Sciences, ul. Koroleva 4, 249036, Obninsk, Russia aut NATIONALLICENCE 700 1- Mandrugin A. Faculty of Chemistry, Lomonosov Moscow State University, 119992, Moscow, Russia aut NATIONALLICENCE 700 1- Fedoseev V. Faculty of Chemistry, Lomonosov Moscow State University, 119992, Moscow, Russia aut NATIONALLICENCE 773 0- Biochemistry (Moscow) Nauka/Interperiodica 70/1(2005-01-01), 8-23 0006-2979 70:1<8 2005 70 10541 NATIONALLICENCE 856 40 https://doi.org/10.1007/s10541-005-0048-9 text/html Onlinezugriff via DOI Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer NATIONALLICENCE NATIONALLICENCE NL-springer