Discovery of a novel nonphosphorylated pentapeptide motif displaying high affinity for Grb2-SH2 domain by the utilization of 3'-substituted tyrosine derivatives

…, ML Peach, PP Roller, S Qiu, S Wang…

Index: Song, Yan-Li; Peach, Megan L.; Roller, Peter P.; Qiu, Su; Wang, Shaomeng; Long, Ya-Qiu Journal of Medicinal Chemistry, 2006 , vol. 49, # 5 p. 1585 - 1596

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Citation Number: 36

Abstract

The growth factor receptor-bound protein 2 (Grb2) is an SH2 domain-containing docking module that represents an attractive target for anticancer therapeutic intervention. An impressive number of synthetic Grb2-SH2 domain inhibitors have been identified; however, clinical agents operating by this mechanism are lacking, due in part to the unique requirement of anionic phosphate-mimicking functionality for high SH2 domain-binding ...