オバタケ　キヨウコ
  大畠　京子
   所属   薬学部 薬学科
   職種   教授
言語種別 英語
発行・発表の年月 2014/12
形態種別 学術論文
査読 査読あり
標題 Iminosugar-Based Galactoside Mimics as Inhibitors of Galactocerebrosidase: SAR Studies and Comparison with Other Lysosomal Galactosidases.
執筆形態 共著
掲載誌名 ChemMedChem.
巻・号・頁 9(12),pp.2647-2652
著者・共著者 Biela-Banaś A., Oulaïdi F., Front S., Gallienne E., Ikeda-Obatake K., Asano N., Wenger D. A. , Martin O. R.
概要 Several families of iminosugar-based galactoside mimics were designed, synthesized, and evaluated as galactocerebrosidase (GALC) inhibitors. They were also tested as inhibitors of lysosomal beta- and alpha-galactosidases in order to find new potent and selective pharmacological chaperones for treatment of the lysosomal storage disorder, Krabbe disease. Whereas 1-C-alkyl imino-L-arabinitols are totally inactive toward the three enzymes, 1-C-alkyl imino-D-galactitols were found to be active only toward alpha-galactosidase A. Finally, 1-N-iminosugars provided the best results, as 4-epi-isofagomine was found to be a good inhibitor of both lysosomal beta-galactosidase and GALC. Further elaboration of this structure is required to achieve selectivity between these two galactosidases.