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American Chemical Society, Journal of Medicinal Chemistry, 9(56), p. 3710-3724, 2013

DOI: 10.1021/jm4002583

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Structural, Kinetic, and Pharmacodynamic Mechanisms of d -Amino Acid Oxidase Inhibition by Small Molecules

Journal article published in 2013 by Seth C. Hopkins, Michele L. R. Heffernan, M. L. R., Lakshmi D. Saraswat, Carrie A. Bowen, Laurence Melnick, Larry W. Hardy, Michael A. Orsini, Michael S. Allen, Patrick Koch, Kerry L. Spear, Robert J. Foglesong, Mustapha Soukri, Milan Chytil, Q. Kevin Fang and other authors.
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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Abstract

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 inhibitors possessed high affinity (Kd ≈ 100-200 nM) and slow release kinetics (k