Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain

…, C Garcia-Echeverria, H Fretz, J Rahuel, P Furet

Index: Schoepfer, Joseph; Gay, Brigitte; Caravatti, Giorgio; Garcia-Echeverria, Carlos; Fretz, Heinz; Rahuel, Joseph; Furet, Pascal Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 20 p. 2865 - 2870

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Citation Number: 23

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.