当前位置: X-MOL 学术Isr. J. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
DNA Encoded Libraries: A Visitor's Guide
Israel Journal of Chemistry ( IF 3.2 ) Pub Date : 2020-01-17 , DOI: 10.1002/ijch.201900133
Dillon T. Flood 1 , Cian Kingston 1 , Julien C. Vantourout 1 , Philip E. Dawson 1 , Phil S. Baran 1
Affiliation  

In 1992, Brenner and Lerner hypothesized that individual chemical transformations could be encoded in DNA, allowing the rapid synthesis and screening of large collections of small molecules. Since their report, huge investments into the development of the DNA encoded library (DEL) technology have enabled the acceleration of the drug discovery process especially early phase discovery undertakings such as target validation and hit identification. As DEL lies at the nexus between chemistry and biology, there is an increasing need to expand the toolboxes of both organic transformations and biological methods. However, the myriad of techniques and reactions already reported can be difficult to digest for practitioners whose expertise resides outside the realm of DEL. This review therefore focuses on a stepwise presentation of DEL from the basic concepts to newest developments. The presentation includes the history, fundamentals, and successes of DEL, different methods for DEL synthesis and affinity selection, the conventional transformations, and finally the latest developments from a synthetic organic perspective.

中文翻译:

DNA编码库:访问者指南

1992年,Brenner和Lerner假设可以在DNA中编码单个化学转化,从而可以快速合成和筛选大量小分子。自从他们的报告以来,对DNA编码文库(DEL)技术发展的巨额投资使加速药物发现过程特别是早期阶段的发现事业如目标验证和命中鉴定成为可能。由于DEL处于化学和生物学之间的关系,因此越来越需要扩展有机转化和生物学方法的工具箱。但是,对于专门知识不在DEL领域之外的从业人员,已经报道的众多技术和反应可能难以消化。因此,本文的重点是从基本概念到最新进展的DEL逐步介绍。演讲内容包括DEL的历史,基本原理和成功经验,DEL合成和亲和力选择的不同方法,常规转化,以及从合成有机视角出发的最新进展。
更新日期:2020-01-17
down
wechat
bug