Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2

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• 作者：Caravatti ; Giorgio ; Rahuel ; Joseph ; Gay ; Brigitte ; Furet ; Pascal
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1999
• 出版时间：July 19, 1999
• 年：1999
• 卷：9
• 期：14
• 页码：1973-1978
• 全文大小：268 K

文摘

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.