Author/Authors :
Joseph Schoepfer، نويسنده , , Heinz Fretz، نويسنده , , Brigitte Gay، نويسنده , , Pascal Furet، نويسنده , , Carlos Garcia-Echeverria، نويسنده , , Nicole End، نويسنده , , Giorgio Caravatti، نويسنده ,
Abstract :
Highly potent inhibitors of the Grb2-SH2 domain have been synthesized. They share the common sequence: Ac-Pmp-Ac6c-Asn-NH-(3-indolyl-propyl). Different substituents at the 3-indolyl-propylamine C-terminal group were explored to further improve the activity. This is the first example of inhibitors of SH2 domains with sub-nanomolar affinity reported to date.
