Bioorganic and Medicinal Chemistry Letters p. 1973 - 1978 (1999)
Update date:2022-08-04
Topics:
Caravatti, Giorgio
Rahuel, Joseph
Brigitte, Gay
Furet, Pascal
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.
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Doi:10.1016/S0022-328X(99)00216-8
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