Journal of Biological Chemistry p. 12873 - 12881 (2010)
Update date:2022-08-29
Topics:
Smith, Myron A.
Mack, Volker
Ebneth, Andreas
Moraes, Isabel
Felicetti, Brunella
Wood, Michael
Schonfeld, Dorian
Mather, Owen
Cesura, Andrea
Barker, John
Serine racemase is responsible for the synthesis of D-serine, an endogenous co-agonist for N-methyl-D-aspartate receptor-type glutamate receptors (NMDARs). This pyridoxal 5′-phosphate-dependent enzyme is involved both in the reversible conversion of L- to D-serine and serine catabolism by α,β-elimination of water, thereby regulating D-serine levels. Because D-serine affects NMDAR signaling throughout the brain, serine racemase is a promising target for the treatment of disorders related to NMDAR dysfunction. To provide a molecular basis for rational drug design the x-ray crystal structures of human and rat serine racemase were determined at 1.5- and 2.1-A resolution, respectively, and in the presence and absence of the orthosteric inhibitor malonate. The structures revealed a fold typical of β-family pyridoxal 5′-phosphate enzymes, with both a large domain and a flexible small domain associated into a symmetric dimer, and indicated a ligand-induced rearrangement of the small domain that organizes the active site for specific turnover of the substrate.
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