Author/Authors :
Charles J. Stankovic، نويسنده , , Narayanan Surendran، نويسنده , , Elizabeth A. Lunney، نويسنده , , Mark S. Plummer، نويسنده , , Kimberly S. Para، نويسنده , , Aurash Shahripour، نويسنده , , James H. Fergus، نويسنده , , James S. Marks MD MPH، نويسنده , , Roman Herrera، نويسنده , , Susan E. Hubbell، نويسنده , , Christine Humblet، نويسنده , , Alan R. Saltiel، نويسنده , , Barbra H. Stewart، نويسنده , , Tomi K. Sawyer، نويسنده ,
Abstract :
Incorporation of 4-phosphonodifluoromethyl-phenylalanine (F2Pmp) and 4-phosphono-phenylalanine into SH2 targeted peptides and peptidomimetic ligands was found to effect binding affinity and selectivity of these ligands toward the Src and Abl SH2 domains. Furthermore, dipeptide analogs containing these phosphonate amino acids were used to produce prodrugs with excellent cellular delivery and reconversion rates.