Synthesis and Characterization of Intermediate and Transition-State Analogue Inhibitors of γ-Glutamyl Peptide Ligases

• INOUE Makoto

  Institute for Chemical Research, Kyoto University

• HIRATAKE Jun

  Institute for Chemical Research, Kyoto University

• SAKATA Kanzo

  Institute for Chemical Research, Kyoto University

書誌事項

タイトル別名

• Synthesis and Characterization of Intermediate and Transition-State Analogue Inhibitors of .GAMMA.-Glutamyl Peptide Ligases.
• Synthesis and Characterization of Intermediate and Transition-State Analogue Inhibitors of ガンマーGlutamyl Peptide Ligases

抄録

  The phosphonodifluoromethyl ketone and phosphonofluoridate derivatives of L-glutamic acid were synthesized and characterized as analogues of the γ-glutamyl phosphate intermediate and the tetrahedral transition state, respectively, for the inhibition of γ-glutamylcysteine synthetase and glutamine synthetase. The former served as a poor inhibitor of both enzymes, but the latter inhibited glutamine synthetase with a K_i of 59 μM and partially inactivated the enzyme in an NH₃- and ATP-dependent manner.<br>

収録刊行物

• Ｂｉｏｓｃｉｅｎｃｅ，　Ｂｉｏｔｅｃｈｎｏｌｏｇｙ，　ａｎｄ　Ｂｉｏｃｈｅｍｉｓｔｒｙ

  Ｂｉｏｓｃｉｅｎｃｅ，　Ｂｉｏｔｅｃｈｎｏｌｏｇｙ，　ａｎｄ　Ｂｉｏｃｈｅｍｉｓｔｒｙ 63 (12), 2248-2251, 1999

  公益社団法人 日本農芸化学会

キーワード

• γ-glutamyl peptide ligase
• intermediate analogue
• transition-state analogue
• phosphonodifluoromethyl ketone
• phosphonofluoridate

詳細情報

• CRID: 1390001206474368128
• NII論文ID: 110002679455
• NII書誌ID: AA10824164
• DOI: 10.1271/bbb.63.2248
• COI: 1:CAS:528:DC%2BD3cXlsFKruw%3D%3D
• ISSN: 13476947
• ISSN: 09168451
• NDL書誌ID: 4949005
• PubMed: 10664863
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I4949005
• Web Site: http://www.tandfonline.com/doi/pdf/10.1271/bbb.63.2248
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可