DNA-encoded chemical libraries: foundations and applications in lead discovery

被引：108

作者：

Zimmermann, Gunther ^{[1
]}

Neri, Dario ^{[1
]}

机构：

[1] Swiss Fed Inst Technol, Dept Chem & Appl Biosci, Vladimir Prelog Weg 1-5-10, CH-8093 Zurich, Switzerland

来源：

DRUG DISCOVERY TODAY | 2016年 / 21卷 / 11期

基金：

瑞士国家科学基金会;

关键词：

SMALL-MOLECULE LIBRARIES; COMBINATORIAL CHEMISTRY; TEMPLATED SYNTHESIS; IN-VITRO; INHIBITORS; SELECTION; IDENTIFICATION; DISPLAY; TARGETS; POTENT;

D O I：

10.1016/j.drudis.2016.07.013

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

DNA-encoded chemical libraries have emerged as a powerful tool for hit identification in the pharmaceutical industry and in academia. Similar to biological display techniques (such as phage display technology), DNA-encoded chemical libraries contain a link between the displayed chemical building block and an amplifiable genetic barcode on DNA. Using routine procedures, libraries containing millions to billions of compounds can be easily produced within a few weeks. The resulting compound libraries are screened in a single test tube against proteins of pharmaceutical interest and hits can be identified by PCR amplification of DNA barcodes and subsequent high-throughput sequencing.

引用

页码：1828 / 1834

页数：7

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