Selective inhibition of Src protein tyrosine kinase by analogues of 5- S-glutathionyl-β-alanyl-L-dopa

Article abstract of DOI:10.1248/cpb.46.1950

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).

Full text of DOI:10.1248/cpb.46.1950

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