TAILIEUCHUNG - Báo cáo khoa học: Relationship between the structure of guanidines and N-hydroxyguanidines, their binding to inducible nitric oxide synthase (iNOS) and their iNOS-catalysed oxidation to NO

The binding of several alkyl- and aryl-guanidines andN-hydroxyguanidines to the oxygenase domain of inducible NO-synthase (iNOSoxy) was studied by UV⁄Vis difference spectroscopy. In a very general manner, monosubsti-tuted guanidines exhibited affinities for iNOSoxy that were very close to those of the corresponding N-hydroxyguanidines. The highest affinities were observed for the natural substrates,l-arginine and N x -hydroxy-l-arginine (Kd at thelmlevel). | iFEBS Journal Relationship between the structure of guanidines and W-hydroxyguanidines their binding to inducible nitric oxide synthase iNOS and their iNOS-catalysed oxidation to NO David Lefevre-Groboillot1 2 Jean-Luc Boucher1 Dennis J. Stuehr2 and Daniel Mansuy1 1 Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques Universite Paris 5 France 2 Department of Immunology Lerner Research Institute Cleveland OH USA Keywords binding kinetic guanidines N-hydroxyguanidines nitric oxide synthase UV Vis difference spectroscopy Correspondence J-L. Boucher Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques UMR 8601 CNRS Universite Paris 5 45 rue des Saints-Peres 75270 Paris Cedex 06 France Fax 33 1 42 86 83 87 Tel 33 1 42 86 21 91 E-mail boucher@ Received 18 February 2005 revised 20 April2005 accepted 25 April 2005 doi The binding of several alkyl- and aryl-guanidines and N-hydroxyguanidines to the oxygenase domain of inducible NO-synthase iNOSoxy was studied by UV Vis difference spectroscopy. In a very general manner monosubstituted guanidines exhibited affinities for iNOSoxy that were very close to those of the corresponding N-hydroxyguanidines. The highest affinities were observed for the natural substrates L-arginine and N -hydroxy-L-arginine Kd at the IM level . The deletion of either the CO2H or the NH2 function of their amino acid moiety led to dramatic decreases in the affinity. However alkylguanidines with a relatively small alkyl chain exhibited interesting affinities the best being observed for a butyl chain Kd 20 M . Arylguanidines also bound to iNOSoxy however with lower affinities Kd 250 IM . Many N-alkyl- and N-aryl-N -hydroxyguanidines are oxidized by iNOS with formation of NO whereas only few alkylguanidines led to significant production of NO under identical conditions and all the arylguanidines tested to date were unable to lead to the production of NO. The kcat

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