Cyclic phosphopeptides for interference with Grb2 SH2 domain signal transduction prepared by ring-closing metathesis and phosphorylation

被引：29

作者：

Dekker, FJ ^{[1
]}

de Mol, NJ ^{[1
]}

Fischer, MJE ^{[1
]}

Kemmink, J ^{[1
]}

Liskamp, RMJ ^{[1
]}

机构：

[1] Univ Utrecht, Dept Med Chem, Utrecht Inst Pharmaceut Sci, NL-3508 TB Utrecht, Netherlands

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2003年 / 1卷 / 19期

关键词：

D O I：

10.1039/b306681a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cyclic phosphopeptides were prepared using ring-closing metathesis followed by phosphorylation. These cyclic phosphopeptides were designed to interact with the SH2 domain of Grb2, which is a signal transduction protein of importance as a target for antiproliferative drug development. Binding of these peptides to the Grb2 SH2 domain was evaluated by a surface plasmon resonance assay. High affinity binding to the Grb2 SH2 domain was maintained upon macrocyclization, thus indicating that this method can be used to assemble high affinity cyclic phosphopeptides that interfere with signal transduction cascades.

引用

页码：3297 / 3303

页数：7

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