| 10819990 |
Wang W, Ramdas L, Sun G, Ke S, Obeyesekere NU, Budde RJ, McMurray JS: Cyclic peptides incorporating 4-carboxyphenylalanine and phosphotyrosine are potent inhibitors of pp60 (c-)(src). Biochemistry. 2000 May 2;39(17):5221-8.
Of these, 4-carboxyphenylalanine (4-Cpa) and phosphotyrosine resulted in high affinity peptides exhibiting K (i) values of 0.85 and 1.1 microM, respectively, 180- and 130-fold increases in potency over the parent cyclic peptide (K (i) = 150 microM).
Furthermore, the 4-Cpa-containing cyclic decapeptide shows remarkable selectivity in the inhibition of Src versus the src family members Yes and Lck, as well as other protein tyrosine kinases, Ser/Thr kinases, and other ATP-utilizing enzymes. |
1(0,0,0,1) |
Details |