DNA-Controlled Bivalent Presentation of Ligands for the Estrogen Receptor

被引：56

作者：

Abendroth, Frank ^{[1
]}

Bujotzek, Alexander ^{[2
]}

Shan, Min ^{[3
]}

Haag, Rainer ^{[3
]}

Weber, Marcus ^{[2
]}

Seitz, Oliver ^{[1
]}

机构：

[1] Humboldt Univ, Inst Chem, D-12489 Berlin, Germany

[2] Zuse Inst Berlin, Berlin, Germany

[3] FU Berlin, Inst Chem & Biochem, Berlin, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2011年 / 50卷 / 37期

关键词：

click chemistry; drug discovery; multivalency; receptors; steroid hormones; BINDING; DIMERIZATION; TAMOXIFEN; DOMAIN; SITE;

D O I：

10.1002/anie.201101655

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Molecular ruler: Steroid analogues were conjugated to DNA by using click chemistry, and self-assembly provided ternary DNA complexes with bivalent ligand presentation. The distance between the bound ligands was measured by spatial screening of the estrogen receptor, and a second hydrophobic binding site was postulated. The picture shows the DNA(black)-raloxifene(orange) complex in the ligand binding domain of the receptor. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

收藏

页码：8592 / 8596

页数：5

相关论文

共 51 条

[1] Assembling materials with DNA as the guide [J].

Aldaye, Faisal A. ;

Palmer, Alison L. ;

Sleiman, Hanadi F. .

SCIENCE, 2008, 321 (5897) :1795-1799

[2] Organization of 'nanocrystal molecules' using DNA [J].

Alivisatos, AP ;

Johnsson, KP ;

Peng, XG ;

Wilson, TE ;

Loweth, CJ ;

Bruchez, MP ;

Schultz, PG .

NATURE, 1996, 382 (6592) :609-611

[3]

[Anonymous], 2011, ANGEW CHEM, DOI DOI 10.1002/ANGE.201007593

[4] DNA as supramolecular scaffold for functional molecules: progress in DNA nanotechnology [J].

Bandy, Thomas J. ;

Brewer, Ashley ;

Burns, Jonathan R. ;

Marth, Gabriella ;

Nguyen, ThaoNguyen ;

Stulz, Eugen .

CHEMICAL SOCIETY REVIEWS, 2011, 40 (01) :138-148

[5] BIVALENT LIGANDS AS PROBES OF ESTROGEN-RECEPTOR ACTION [J].

BERGMANN, KE ;

WOOGE, CH ;

CARLSON, KE ;

KATZENELLENBOGEN, BS ;

KATZENELLENBOGEN, JA .

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1994, 49 (2-3) :139-152

[6] DNA-templated assembly and electrode attachment of a conducting silver wire [J].

Braun, E ;

Eichen, Y ;

Sivan, U ;

Ben-Yoseph, G .

NATURE, 1998, 391 (6669) :775-778

[7] Molecular basis of agonism and antagonism in the oestrogen receptor [J].

Brzozowski, AM ;

Pike, ACW ;

Dauter, Z ;

Hubbard, RE ;

Bonn, T ;

Engstrom, O ;

Ohman, L ;

Greene, GL ;

Gustafsson, JA ;

Carlquist, M .

NATURE, 1997, 389 (6652) :753-758

[8] Towards a rational spacer design for bivalent inhibition of estrogen receptor [J].

Bujotzek, Alexander ;

Shan, Min ;

Haag, Rainer ;

Weber, Marcus .

JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 2011, 25 (03) :253-262

[9] Polytriazoles as copper(I)-stabilizing ligands in catalysis [J].

Chan, TR ;

Hilgraf, R ;

Sharpless, KB ;

Fokin, VV .

ORGANIC LETTERS, 2004, 6 (17) :2853-2855

[10]

Chang CY, 1999, MOL CELL BIOL, V19, P8226

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