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

共 50 条

[41] Fully flexible docking models of the complex between α7 nicotinic receptor and a potent heptapeptide inhibitor of the β-amyloid peptide binding
Espinoza-Fonseca, L. Michel
Trujillo-Ferrara, Jose G.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (13) : 3519 - 3523
[42] Development of Photoswitchable Estrogen Receptor Ligands
Tsuchiya, Keisuke
Umeno, Tomohiro
Tsuji, Genichiro
Yokoo, Hidetomo
Tanaka, Masakazu
Fukuhara, Kiyoshi
Demizu, Yosuke
Misawa, Takashi
[J]. CHEMICAL & PHARMACEUTICAL BULLETIN, 2020, 68 (04) : 398 - 402
[43] Signal Pathway of Estrogen and Estrogen Receptor in the Development of Thyroid Cancer
Liu, Jian
Xu, Tianmin
Ma, Li
Chang, Weiqin
[J]. FRONTIERS IN ONCOLOGY, 2021, 11
[44] Ovarian estrogen receptor α and β mRNA expression:: impact of development and estrogen
Drummond, AE
Baillie, AJ
Findlay, JK
[J]. MOLECULAR AND CELLULAR ENDOCRINOLOGY, 1999, 149 (1-2) : 153 - 161
[45] XR5944 is a potent inhibitor of estrogen receptors through a novel mechanism
Punchihewa, Chandanamali
Carver, Megan
De Alba, Adrian
Sidell, Neil
Yang, Danzhou
[J]. CANCER RESEARCH, 2008, 68 (09)
[46] Retro-inverso peptide inhibitor nanoparticles as potent inhibitors of aggregation of the Alzheimer's Aβ peptide
Gregori, Maria
Taylor, Mark
Salvati, Elisa
Re, Francesca
Mancini, Simona
Balducci, Claudia
Forloni, Gianluigi
Zambelli, Vanessa
Sesana, Silvia
Michael, Maria
Michail, Christos
Tinker-Mill, Claire
Kolosov, Oleg
Sherer, Michael
Harris, Stephen
Fullwood, Nigel J.
Masserini, Massimo
Allsop, David
[J]. NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE, 2017, 13 (02) : 723 - 732
[47] Converting a weak peptide inhibitor of Src kinase to potent peptide inhibitors by systemic structural modification
Kumar, Anil
Wang, Yuehao
Sun, Gongqin
Parang, Keykavous
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2731 - U2732
[48] Potent estrogen receptor ligands based on bisphenols with a globular hydrophobic core
Endo, Y
Yoshimi, T
Ohta, K
Suzuki, T
Ohta, S
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (12) : 3941 - 3944
[49] Asymmetric synthesis of BB-3497 - A potent peptide deformylase inhibitor
Pratt, LM
Beckett, RP
Davies, SJ
Launchbury, SB
Miller, A
Spavold, ZM
Todd, RS
Whittaker, M
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (19) : 2585 - 2588
[50] Aromatic amines as potent inhibitors selective for estrogen receptor a over b
Tan, John Q.
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2013, 245

← 1 2 3 4 5 →