ビタミンB_2誘導体を補酵素とする脳内活性D-アミノ酸代謝酵素の新規阻害剤(<特集>ビタミンB研究委員会平成25年度シンポジウム「ビタミンB群が担う脳内アミノ酸代謝と疾患をターゲットにした次世代学術研究-ビタミン研究が切り拓く疾患生命科学のフロンティア」)

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タイトル別名
  • Novel inhibitors of flavin enzymes that act on bioactive D-amino acids in the mammalian brain
  • ビタミンB₂誘導体を補酵素とする脳内活性D-アミノ酸代謝酵素の新規阻害剤
  • ビタミン B ₂ ユウドウタイ オ ホ コウソ ト スル ノウナイ カッセイ D-アミノサン タイシャ コウソ ノ シンキ ソガイザイ

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抄録

D-Amino acid oxidase (DAO) and D-aspartate oxidase (DDO) are FAD-containing flavoproteins that catalyze the oxidative deamination of D-amino acids, including D-serine, D-alanine and D-aspartate, which are a potential coagonist or agonist of the N-methyl-D-aspartate (NMDA) receptor. Dysfunction of NMDA receptor-mediated neurotransmission has been implicated in the onset of various mental disorders such as schizophrenia. These findings may allow us to think that DAO and DDO inhibitors that can be expected to activate NMDA receptor function by augmenting the brain levels of D-serine, D-alanine and/or D-aspartate become new antipsychotic drugs in the treatment of schizophrenia. Therefore, we have tried to search and identify novel DAO and DDO inhibitors based on screening of manifold biologically active compounds of microbial origin and pre-existing drugs, or in silico screening of a large number of compounds. Herein, we review our recent studies on the compounds identified as DAO or DDO inhibitors.

収録刊行物

  • ビタミン

    ビタミン 88 (9), 469-477, 2014

    公益社団法人 日本ビタミン学会

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