Structure-function relationship in a beta-sheet peptide inhibitor of E47 dimerization and DNA binding.

Ghosh I; Issac R; Chmielewski J

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Structure-function relationship in a beta-sheet peptide inhibitor of E47 dimerization and DNA binding.

机译：Structure-function relationship in a beta-sheet peptide inhibitor of E47 dimerization and DNA binding.

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摘要

A beta-sheet peptide inhibitor, 2H10, has been developed that inhibits the dimerization of the transcription factor E47. Inhibition of E47 dimerization has been demonstrated to also inhibit the DNA binding of this transcription factor. Truncated peptides based on 2H10 have demonstrated that the beta-sheet content of these peptides directly correlates with their inhibitory properties. Individual residues within 2H10 were identified that were responsible for the beta-sheet secondary structure by employing an alanine replacement strategy. The beta-sheet character of the alanine mutants also correlated well with their inhibition of E47 DNA binding. These results provide further evidence that interactions between the interfacial peptide inhibitors of E47 and the transcription factor itself are mediated by a beta-sheet structure.

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来源
《Bioorganic and medicinal chemistry》 |1999年第1期|61-66|共6页
作者
Ghosh I; Issac R; Chmielewski J;
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作者单位

Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.;

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原文格式 PDF
正文语种英语
中图分类药学;生物化学;
关键词
DNA-Binding Proteins; Oligopeptides; Peptides; Protein Structure; Secondary; DNA结合蛋白质类; 寡肽类; 肽类; 蛋白质结构; 二级;

Structure-function relationship in a beta-sheet peptide inhibitor of E47 dimerization and DNA binding.

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