A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells

被引：18

作者：

Hu, Zhiye ^{[1
]}

Yang, Lu ^{[1
]}

Ning, Wentao ^{[1
]}

Tang, Chu ^{[1
]}

Meng, Qiuyu ^{[1
]}

Zheng, Jie ^{[1
]}

Dong, Chune ^{[1
]}

Zhou, Hai-Bing ^{[1
]}

机构：

[1] Wuhan Univ, State Key Lab Virol, Hubei Prov Engn & Technol Res Ctr Fluorinated Pha, Hubei Prov Key Lab Dev Originated Dis,Sch Pharmac, Wuhan 430071, Peoples R China

来源：

CHEMICAL COMMUNICATIONS | 2018年 / 54卷 / 31期

关键词：

ER-BETA; INTERNATIONAL-UNION; CANCER; EXPRESSION; PROSTATE; LIGANDS; ALPHA;

D O I：

10.1039/c8cc00483h

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Estrogen receptor (ER) has recently been identified as a pharmaceutical target in hormone replacement therapy for breast cancers. However, the biological function of ER in disease progression remains unclear. A highly ER-selective fluorescent probe (FPNM) was discovered exhibiting nanomolar affinity for ER with an ER/ER selectivity as high as 80, which allowed specific labeling of intracellular ER. Moreover, distinct ER dynamics in various cellular bio-settings such as prostate cancer (DU-145) or triple-negative breast cancer (MDA-MB-231) cells were directly observed for the first time viaFPNM staining.

引用

收藏

页码：3887 / 3890

页数：4

相关论文

共 34 条

[1] High Affinity Fluorescent Ligands for the Estrogen Receptor [J].

Abendroth, Frank ;

Solleder, Marthe ;

Mangoldt, Dorothea ;

Welker, Pia ;

Licha, Kai ;

Weber, Marcus ;

Seitz, Oliver .

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2015, 2015 (10) :2157-2166

[2] Altered ligand binding properties and enhanced stability of a constitutively active estrogen receptor: Evidence that an open pocket conformation is required for ligand interaction [J].

Carlson, KE ;

Choi, I ;

Gee, A ;

Katzenellenbogen, BS ;

Katzenellenbogen, JA .

BIOCHEMISTRY, 1997, 36 (48) :14897-14905

[3] Diarylpropionitrile (DPN) Enantiomers: Synthesis and Evaluation of Estrogen Receptor β-Selective Ligands [J].

Carroll, Vincent M. ;

Jeyakumar, M. ;

Carlson, Kathryn E. ;

Katzenellenbogen, John A. .

JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (01) :528-537

[4] A water-soluble perylene dye functionalised with a 17β-estradiol: a new fluorescent tool for steroid hormones [J].

Cespedes-Guirao, Francisco J. ;

Ropero, Ana B. ;

Font-Sanchis, Enrique ;

Nadal, Angel ;

Fernandez-Lazaro, Fernando ;

Sastre-Santos, Angela .

CHEMICAL COMMUNICATIONS, 2011, 47 (29) :8307-8309

[5] International Union of Pharmacology.: LXIV.: Estrogen receptors [J].

Dahlman-Wright, Karin ;

Cavailles, Vincent ;

Fuqua, Suzanne A. ;

Jordan, V. Craig ;

Katzenellenbogen, John A. ;

Korach, Kenneth S. ;

Maggi, Adriana ;

Muramatsu, Masami ;

Parker, Malcolm G. ;

Gustafsson, Jan-Ake .

PHARMACOLOGICAL REVIEWS, 2006, 58 (04) :773-781

[6] A fluorescent histone deacetylase (HDAC) inhibitor for cellular imaging [J].

Fleming, Cassandra L. ;

Ashton, Trent D. ;

Nowell, Cameron ;

Devlin, Mark ;

Natoli, Anthony ;

Schreuders, Jeannette ;

Pfeffer, Frederick M. .

CHEMICAL COMMUNICATIONS, 2015, 51 (37) :7827-7830

[7] Triple-Negative Breast Cancer [J].

Foulkes, William D. ;

Smith, Ian E. ;

Reis-Filho, Jorge S. .

NEW ENGLAND JOURNAL OF MEDICINE, 2010, 363 (20) :1938-1948

[8] Estrogen Receptor Beta in Cancer: an Attractive Target for Therapy [J].

Gallo, Daniela ;

De Stefano, Ilaria ;

Prisco, Maria Grazia ;

Scambia, Giovanni ;

Ferrandina, Gabriella .

CURRENT PHARMACEUTICAL DESIGN, 2012, 18 (19) :2734-2757

[9] Fluorescent chemical probes for accurate tumor diagnosis and targeting therapy [J].

Gao, Min ;

Yu, Fabiao ;

Lv, Changjun ;

Choo, Jaebum ;

Chen, Lingxin .

CHEMICAL SOCIETY REVIEWS, 2017, 46 (08) :2237-2271

[10] A Bright Future for Precision Medicine: Advances in Fluorescent Chemical Probe Design and Their Clinical Application [J].

Garland, Megan ;

Yim, Joshua J. ;

Bogyo, Matthew .

CELL CHEMICAL BIOLOGY, 2016, 23 (01) :122-136

← 1 2 3 4 →