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Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2
1Novartis Pharmaceuticals, Inc., Therapeutic Area Oncology, Basel, Switzerland.
Bioorganic & Medicinal Chemistry Letters
|August 18, 1999
Abstract:
The structure-based design and synthesis of a completely non-peptidic, micromolar antagonist of the SH2 domain of Grb2 is presented. The compound mimics the two main pharmacophores of the natural ligand, the phenylphosphate of the phosphotyrosine residue and the beta-carboxamide of the X+2 asparagine, which are linked by a rigid aromatic spacer.