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Highly potent inhibitors of the Grb2-SH2 domain
1Novartis Pharma Inc., Oncology Research Department, Basle, Switzerland. joseph.schoepfer@pharma.novartis.com
Bioorganic & Medicinal Chemistry Letters
|February 18, 1999
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.