Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2

G Caravatti, J Rahuel, B Gay, P Furet

文献索引：Caravatti, Giorgio; Rahuel, Joseph; Brigitte, Gay; Furet, Pascal Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 14 p. 1973 - 1978

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被引用次数: 22

摘要

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 β-carboxamide of the X+ 2 asparagine, which are linked by a rigid aromatic spacer.