Highly potent inhibitors of the Grb2-SH2 domain

…, H Fretz, B Gay, P Furet, C García-Echeverría…

Index: Schoepfer, Joseph; Fretz, Heinz; Gay, Brigitte; Furet, Pascal; Garcia-Echeverria, Carlos; End, Nicole; Caravatti, Giorgio Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 221 - 226

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Citation Number: 55

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.