Preparation of Small-Molecule Microarrays by trans-Cyclooctene Tetrazine Ligation and Their Application in the High-Throughput Screening of Protein-Protein Interaction Inhibitors of Bromodomains

被引：34

作者：

Zhang, Chong-Jing ^{[1
]}

Tan, Chelsea Y. J. ^{[1
]}

Ge, Jingyan ^{[1
]}

Na, Zhenkun ^{[1
]}

Chen, Grace Y. J. ^{[1
]}

Uttamchandani, Mahesh ^{[1
]}

Sun, Hongyan ^{[2
]}

Yao, Shao Q. ^{[1
]}

机构：

[1] Natl Univ Singapore, Dept Chem, Singapore 117543, Singapore

[2] City Univ Hong Kong, Dept Biol & Chem, Hong Kong, Hong Kong, Peoples R China

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2013年 / 52卷 / 52期

基金：

英国医学研究理事会;

关键词：

bioorthogonal chemistry; epigenetics; inhibitors; protein-protein interactions; small-molecule microarrays; DISCOVERY; PEPTIDE; BINDING; TOOLS;

D O I：

10.1002/anie.201307803

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Fast and efficient: A library of trans-cyclooctene (TCO)-modified small molecules were immobilized on tetrazine-functionalized glass slides by using the fastest bioorthogonal reaction known. The resulting small-molecule microarray was screened against a variety of human bromodomains to identify protein-protein interaction inhibitors. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：14060 / 14064

页数：5

共 39 条

[1] Small-molecule inhibitors of protein-protein interactions: Progressing towards the dream [J].

Arkin, MR ;

Wells, JA .

NATURE REVIEWS DRUG DISCOVERY, 2004, 3 (04) :301-317

[2] Epigenetic protein families: a new frontier for drug discovery [J].

Arrowsmith, Cheryl H. ;

Bountra, Chas ;

Fish, Paul V. ;

Lee, Kevin ;

Schapira, Matthieu .

NATURE REVIEWS DRUG DISCOVERY, 2012, 11 (05) :384-400

[3] Preparation of Carbohydrate Arrays by Using Diels-Alder Reactions with Inverse Electron Demand [J].

Beckmann, Henning S. G. ;

Niederwieser, Andrea ;

Wiessler, Manfred ;

Wittmann, Valentin .

CHEMISTRY-A EUROPEAN JOURNAL, 2012, 18 (21) :6548-6554

[4] BET domain co-regulators in obesity, inflammation and cancer [J].

Belkina, Anna C. ;

Denis, Gerald V. .

NATURE REVIEWS CANCER, 2012, 12 (07) :465-477

[5] The complex language of chromatin regulation during transcription [J].

Berger, Shelley L. .

NATURE, 2007, 447 (7143) :407-412

[6]

Chung C., 2012, DRUG DISCOV TODAY, V9, pe111, DOI DOI 10.1016/J.DDSTR.2011.12.002

[7] Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery [J].

Chung, Chun-wa ;

Dean, Anthony W. ;

Woolven, James M. ;

Bamborough, Paul .

JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (02) :576-586

[8] Progress in the Discovery of Small-Molecule Inhibitors of Bromodomain-Histone Interactions [J].

Chung, Chun-Wa ;

Witherington, Jason .

JOURNAL OF BIOMOLECULAR SCREENING, 2011, 16 (10) :1170-1185

[9] BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc [J].

Delmore, Jake E. ;

Issa, Ghayas C. ;

Lemieux, Madeleine E. ;

Rahl, Peter B. ;

Shi, Junwei ;

Jacobs, Hannah M. ;

Kastritis, Efstathios ;

Gilpatrick, Timothy ;

Paranal, Ronald M. ;

Qi, Jun ;

Chesi, Marta ;

Schinzel, Anna C. ;

McKeown, Michael R. ;

Heffernan, Timothy P. ;

Vakoc, Christopher R. ;

Bergsagel, P. Leif ;

Ghobrial, Irene M. ;

Richardson, Paul G. ;

Young, Richard A. ;

Hahn, William C. ;

Anderson, Kenneth C. ;

Kung, Andrew L. ;

Bradner, James E. ;

Mitsiades, Constantine S. .

CELL, 2011, 146 (06) :903-916

[10]

Devaraj N. K., 2009, Angew. Chem, V121, P7147, DOI [10.1002/ange.200903233, DOI 10.1002/ANGE.200903233]

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