Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands

…, M Zhang, T Araki, LR Roberts, KM Worthy…

文献索引：Shi, Zhen-Dan; Wei, Chang-Qing; Lee, Kyeong; Liu, Hongpeng; Zhang, Manchao; Araki, Toshiyuki; Roberts, Lindsey R.; Worthy, Karen M.; Fisher, Robert J.; Neel, Benjamin G.; Kelley, James A.; Yang, Dajun; Burke Jr., Terrence R. Journal of Medicinal Chemistry, 2004 , vol. 47, # 8 p. 2166 - 2169

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被引用次数: 34

摘要

Macrocyclization from the phosphotyrosyl (pTyr) mimetic's β-position has previously been shown to enhance Grb2 SH2 domain-binding affinity of phosphonate-based analogues. The current study examined the effects of such macrocyclization using a dicarboxymethyl-based pTyr mimetic. In extracellular assays affinity was enhanced approximately 5-fold relative to an open-chain congener. Enhancement was also observed in whole-cell assays ...