Selective Inhibition of Src Protein Tyrosine Kinase by Analogues of 5-S-Glutathionyl-β-alanyl-L-dopa

  • ZHENG Zhe-bin
    Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
  • NAGAI Sachie
    Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
  • IWANAMI Naoko
    Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
  • KOBAYASHI Ayako
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • HIJIKATA Mariko
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • NATORI Shunji
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • SANKAWA Ushio
    Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

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Abstract

Twelve analogues of the antibacterial phenolic peptide 5-S-glutathionyl-β-alanyl-L-dopa (5-S-GA-L-D : 1) were synthesized via orthoquinones using tyrosinase. Several synthesized compounds inhibited the v-Src autophosphorylation tyrosine kinase reaction with an IC_<50> value comparable to that of herbimycin. The inhibition of c-Src substrate phosphorylation was much less active than v-Src autophosphorylation inhibition. The analogues showed no effects on substrate phosphorylation by epidermal growth factor receptor (EGFR), and this selectivity is the most characteristic feature of the analogues (1-12).

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