Development of a potent peptide inhibitor of estrogen receptor α

被引：0

作者：

Xuan Qin ^{[1
]}

Hui Zhao ^{[1
]}

Yanhong Jiang ^{[1
]}

Feng Yin ^{[1
]}

Yuan Tian ^{[2
]}

Mingsheng Xie ^{[1
]}

Xiyang Ye ^{[3
]}

Naihan Xu ^{[4
]}

Zigang Li ^{[1
]}

机构：

[1] School of Chemical Biology and Biotechnology,Shenzhen Graduate School of Peking University

[2] School of Life Science and Engineering,Southwest Jiaotong University

[3] Department of Gynecology,The Second Clinical Medical College of Jinan University,Shenzhen People's Hospital

[4] Key Lab in Healthy Science and Technology, Division of Life Science,Shenzhen Graduate School of Tsinghua University

来源：

Chinese Chemical Letters | 2018年 / 29卷 / 07期

基金：

中国国家自然科学基金;

关键词：

Peptide inhibitor; TD strategy; N-terminus helix-nucleating strategy; Estrogen receptor α; Cell penetrating peptide;

D O I：

暂无

中图分类号：

TQ464.7 [氨基酸、肽、蛋白质];

学科分类号：

100705 ;

摘要：

We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological applications. A potent peptide inhibitor of estrogen receptor α(ER-α) with significantly increased cellular uptake and cellular distribution was developed by cell penetrating peptide attachment.The resulted peptide conjugate showed selective toxicity towards estrogen receptor positive cell lines and induced decreased transcription of estrogen receptor a downstream genes.

引用

页码：1160 / 1162

页数：3

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