641638-38-2Relevant academic research and scientific papers
Macrocyclization in the Design of Non-Phosphorus-Containing Grb2 SH2 Domain-Binding Ligands
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.
, p. 2166 - 2169 (2007/10/03)
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 examining blockade of Grb2 binding to the erbB-2 protein-tyrosine kinase.
