Author/Authors :
Joseph Schoepfer، نويسنده , , Brigitte Gay، نويسنده , , Giorgio Caravatti، نويسنده , , Carlos Garcia-Echeverria، نويسنده , , Heinz Fretz، نويسنده , , Joseph Rahuel، نويسنده , , Pascal Furet، نويسنده ,
Abstract :
We have designed and synthesized a (3-aminomethyl-phenyl)-urea scaffold to mimic the X+1-Asn part of the minimal phosphopeptide sequence, Ac-pTyr-X+1-Asn-NH2, recognized by the Grb2-SH2 domain. The resulting compounds show the same degree of affinity as their peptide counterparts for the Grb2-SH2 domain. This is the first example reported to date of ligands of the Grb2-SH2 domain with substantially reduced peptidic character.