Citation: Qin Xuan, Zhao Hui, Jiang Yanhong, Yin Feng, Tian Yuan, Xie Mingsheng, Ye Xiyang, Xu Naihan, Li Zigang. Development of a potent peptide inhibitor of estrogen receptor α[J]. Chinese Chemical Letters, ;2018, 29(7): 1160-1162. doi: 10.1016/j.cclet.2018.04.004 shu

Development of a potent peptide inhibitor of estrogen receptor α

Qin Xuan ^a,1 ,
Zhao Hui ^a,1 ,
Jiang Yanhong ^a ,
Yin Feng ^a ,
Tian Yuan ^b ,
Xie Mingsheng ^a ,
Ye Xiyang ^c ,
Xu Naihan ^d ,
Li Zigang ^a,,

a.
School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen 518055, China
b.
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 611756, China
c.
Department of Gynecology, The Second Clinical Medical College of Jinan University, Shenzhen People's Hospital, Shenzhen 518020, China
d.
Key Lab in Healthy Science and Technology, Division of Life Science, Shenzhen Graduate School of Tsinghua University, Shenzhen 518055, China

Corresponding author: Li Zigang, lizg@pkusz.edu.cn

Received Date: 20 January 2018
Revised Date: 15 March 2018
Accepted Date: 19 March 2018
Available Online: 4 July 2018

Figures(4)

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 α downstream genes.
- Peptide inhibitor,
- TD strategy,
- N-terminus helix-nucleating strategy,
- Estrogen receptor α,
- Cell penetrating peptide
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