Inhibition Effects of 5-S-Glutahionyl-N-β-alanyl-L-dopa Analogues against Src Protein Tyrosine Kinase

概要

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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 IC_<50> 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-GA-L-D (1) and its analogous competed with peptide substrate and non-competed with ATP. The analogues showed no effects on substrate phosphorylation by epidermal crowth factor receptor (EGFR), and this selectivity is the most charagteristic feature of the 5-S-GA-L-D and its analogues (1-12).
公益社団法人日本薬学会の論文
1999-06-15