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

DOI: 10.1016/S0960-894X(99)00299-1

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1973 - 1978 (1999)

Update date:2022-08-04

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Authors:

Caravatti, Giorgio

Rahuel, Joseph

Brigitte, Gay

Furet, Pascal

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Article abstract of DOI:10.1016/S0960-894X(99)00299-1

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.

Full text of DOI:10.1016/S0960-894X(99)00299-1

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