| 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.
To test this hypothesis, a series of phenylalanine analogues were substituted at position 7 (the Y + 3 residue) in cyclo (Asp (1)-Asn (2)-Glu (3)-Tyr (4)-Ala (5)-Phe (6)-Phe (7)-Gln (8)-D-Phe (9 )-Pro (10)).
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). |
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