Chemical and Pharmaceutical Bulletin p. 1950 - 1951 (1998)
Update date:2022-09-26
Topics:
Zheng, Zhe-Bin
Nagai, Sachie
Iwanami, Naoko
Kobayashi, Ayako
Hijikata, Mariko
Natori, Shunji
Sankawa, Ushio
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 IC50 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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