Development of peptide antagonists that target estrogen receptor-cofactor interactions

被引：35

作者：

McDonnell, DP ^{[1
]}

Chang, CY ^{[1
]}

Norris, JD ^{[1
]}

机构：

[1] Duke Univ, Med Ctr, Dept Pharmacol & Canc Biol, Durham, NC 27710 USA

来源：

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY | 2000年 / 74卷 / 05期

关键词：

peptide antagonists; estrogen; receptor-cofactor interaction; transcriptional activity;

D O I：

10.1016/S0960-0760(00)00109-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We have developed a series of high-affinity peptide antagonists that inhibit the transcriptional activity of both subtypes of the human estrogen receptor (ER alpha and ER beta). We believe that it will be possible to develop these peptides, or corresponding peptidomimetic derivatives, into pharmaceuticals for use in the treatment of breast cancer and other estrogenopathies. It is anticipated that drugs of this type could be used in combination with classical antiestrogens, such as tamoxifen, to achieve a complete blockage of ER-transcriptional activity. Although ER has been the primary target of our studies to date, it is likely that the insights gained from this work will apply to other nuclear receptors and transcription factors. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：327 / 335

页数：9

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