Art

J-GLOBAL ID：201602246292133115   Reference number：16A1067720

Phosphonate-based irreversible inhibitors of human γ-glutamyl transpeptidase (GGT). GGsTop is a non-toxic and highly selective inhibitor with critical electrostatic interaction with an active-site residue Lys562 for enhanced inhibitory activity

ヒトγ-グルタミルトランスペプチダーゼ(GGT)のホスホン酸エステルの不可逆的阻害剤 GGsTopは阻害活性増強のために活性部位残基Lys562との重要な静電相互作用を有する非毒性かつ高度に選択的な阻害剤である

Author (12)： Kamiyama Akane (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan) ,  Nakajima Mado (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan) ,  Han Liyou (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan) ,  Wada Kei (Organization for Promotion of Tenure Track, University of Miyazaki, 5200 Kihara, Kiyotake, Miyazaki 889-1692, Japan) ,  Mizutani Masaharu (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan) ,  Tabuchi Yukiko (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan) ,  Kojima-Yuasa Akiko (Department of Food and Human Health Sciences, Graduate School of Human Life Science, Osaka City University, 3-3-138 Sugimoto, Sumiyoshi-ku, Osaka 558-8585, Japan) ,  Matsui-Yuasa Isao (Department of Food and Human Health Sciences, Graduate School of Human Life Science, Osaka City University, 3-3-138 Sugimoto, Sumiyoshi-ku, Osaka 558-8585, Japan) ,  Suzuki Hideyuki (Division of Applied Biology, Graduate School of Science and Technology, Kyoto Institute of Technology, Goshokaido-cho, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan) ,  Fukuyama Keiichi (Department of Biological Sciences, Graduate School of Science, Osaka University, Toyonaka, Osaka 560-0043, Japan) ,  Watanabe Bunta (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan) ,  Hiratake Jun (Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan)
Material： Bioorganic & Medicinal Chemistry  (Bioorganic and Medicinal Chemistry)
Volume： 24  Issue： 21  Page： 5340-5352  Publication year： Nov. 01, 2016 
JST Material Number： W0556A  ISSN： 0968-0896  Document type： Article
Article type： 原著論文  Country of issue： Netherlands (NLD)  Language： ENGLISH (EN)

Thesaurus term： *glutamyl transpeptidase ,  *enzyme inhibitor ,  phosphonate ,  enzyme reaction mechanism ,  active site ,  electrostatic interaction ,  amino acid residue ,  Escherichia coli ,  structure-activity relationship ,  X-ray structural analysis ,  crystal structure ,  fibroblast ,  hepatocyte ,  cytotoxicity
Semi thesaurus term： X-ray crystallography ,  hepatic stellate cell

Author keywords (8)： γ-Glutamyl transpeptidase ,  Phosphonate diesters ,  GGsTop ,  Mechanism-based inhibitor ,  Electrostatic interaction ,  Active-site residue Lys562 ,  Selectivity ,  Cytotoxicity

JST classification (2)： Enzyme in general  (EB09010D) ,  Basic research of enzyme preparations and enzyme inhibitor preparations  (GW21010W)

Substance index (1)： 2-Amino-4-[[3-(carboxymethyl)phenoxy]methoxyphosphinyl]butanoic acid

Terms in the title (10)： ヒト ,  γ-グルタミルトランスペプチダーゼ ,  ホスホン酸エステル ,  阻害剤 ,  阻害活性 ,  増強 ,  活性部位 ,  残基 ,  静電相互作用 ,  非毒性