Structural, kinetic, and pharmacodynamic mechanisms of D-amino acid oxidase inhibition by small molecules

We characterized the mechanism and pharmacodynamics of five structurally distinct inhibitors of d-amino acid oxidase. All inhibitors bound the oxidized form of human enzyme with affinity slightly higher than that of benzoate (Kd ≈ 2-4 μM). Stopped-flow experiments showed that pyrrole-based inhibitor...

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Vydáno v:	Journal of medicinal chemistry Ročník 56; číslo 9; s. 3710
Hlavní autoři:	Hopkins, Seth C, Heffernan, Michele L R, Saraswat, Lakshmi D, Bowen, Carrie A, Melnick, Laurence, Hardy, Larry W, Orsini, Michael A, Allen, Michael S, Koch, Patrick, Spear, Kerry L, Foglesong, Robert J, Soukri, Mustapha, Chytil, Milan, Fang, Q Kevin, Jones, Steven W, Varney, Mark A, Panatier, Aude, Oliet, Stephane H R, Pollegioni, Loredano, Piubelli, Luciano, Molla, Gianluca, Nardini, Marco, Large, Thomas H
Médium:	Journal Article
Jazyk:	angličtina
Vydáno:	United States 09.05.2013
Témata:	Animals Behavior, Animal - drug effects Binding, Competitive Catalytic Domain D-Amino-Acid Oxidase - antagonists & inhibitors D-Amino-Acid Oxidase - chemistry D-Amino-Acid Oxidase - metabolism Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Glycine - metabolism Humans Kinetics Male Molecular Docking Simulation Neuroglia - drug effects Neuroglia - metabolism Rats Rats, Sprague-Dawley Serine - biosynthesis Small Molecule Libraries - chemistry Small Molecule Libraries - metabolism Small Molecule Libraries - pharmacokinetics Small Molecule Libraries - pharmacology
ISSN:	1520-4804, 1520-4804
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