Bioorganic and Medicinal Chemistry Letters p. 221 - 226 (1999)
Update date:2022-08-04
Topics:
Schoepfer, Joseph
Fretz, Heinz
Gay, Brigitte
Furet, Pascal
Garcia-Echeverria, Carlos
End, Nicole
Caravatti, Giorgio
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.
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