Inhibition effects of 5-S-glutathionyl-N-β-alanyl-L-dopa analogues against Src protein tyrosine kinase

Article abstract of DOI:10.1248/cpb.47.777

Twelve analogues of the antibacterial phenolic peptide 5-S- glutathionyl-N-β-alanyl-L-dopa (5-S-GA-L-D, 1) were synthesized via orthoquinone using tyrosinase. Several synthesized compounds inhibited the v- Src autophosphorylation tyrosine kinase reaction with an IC₅₀ value comparable to that of herbimycin A. The inhibition of c-Src substrate phosphorylation was much less active than v-Src autophosphorylation inhibition. 5-S-GAL-D (1) and its analogous competed with peptide substrate and non-competed with ATP. The analogues showed no effects on substrate phosphorylation by epidermal growth factor receptor (EGFR), and this selectivity is the most characteristic feature of the 5-S-GA-L-D and its analogues (1 - 12).

Full text of DOI:10.1248/cpb.47.777

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