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J Med Chem. 2004 Apr 8;47(8):2166-9.

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

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1
Laboratory of Medicinal Chemistry, CCR, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, USA.

Abstract

Macrocyclization from the phosphotyrosyl (pTyr) mimetic's beta-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.

PMID:
15056012
DOI:
10.1021/jm030510e
[Indexed for MEDLINE]
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