Title of article
Discovery of highly potent Src SH2 binders: Structure–activity studies and X-ray structures
Author/Authors
Pierre Deprez، نويسنده , , Isabelle Baholet، نويسنده , , Stéphane Burlet، نويسنده , , Gudrun Lange، نويسنده , , Remi Amengual، نويسنده , , Bernard Schoot، نويسنده , , Annie Vermond، نويسنده , , Eliane Mandine، نويسنده , , Dominique Lesuisse، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
1291
To page
1294
Abstract
Optimization of the hydrophobic moiety of caprolactam/thiazepinone based compounds led to the identification of potent Src SH2 binders in two different series incorporating a phosphotyrosine group (RU 81843) or a phosphobenzoic group (RU 79181). The X-ray co-structures with the Src SH2 domain revealed different binding modes for RU 81843 and RU 79181, and an excellent fit between RU81843 and the Src SH2 protein thus explaining its high potency (9 nM, 15-fold more potent than pYEEI reference peptide).
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792198
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