Issue 4, 2021

DNA-encoded libraries (DELs): a review of on-DNA chemistries and their output

Abstract

A DNA-encoded library is a collection of small molecules covalently linked to DNA that has unique information about the identity and the structure of each library member. A DNA-encoded chemical library (DEL) is broadly adopted by major pharmaceutical companies and used in numerous drug discovery programs. The application of the DEL technology is advantageous at the initial period of drug discovery because of reduced cost, time, and storage space for the identification of target compounds. The key points for the construction of DELs comprise the development and the selection of the encoding methods, transfer of routine chemical reaction from off-DNA to on-DNA, and exploration of new chemical reactions on DNA. The limitations in the chemical space and the diversity of DEL were reduced gradually by using novel DNA-compatible reactions based on the formation and the cleavage of various bonds. Here, we summarized a series of novel DNA-compatible chemistry reactions for DEL building blocks and analysed the druggability of screened hit molecules via DELs in the past five years.

Graphical abstract: DNA-encoded libraries (DELs): a review of on-DNA chemistries and their output

Article information

Article type
Review Article
Submitted
21 Nov 2020
Accepted
21 Dec 2020
First published
19 Jan 2021
This article is Open Access
Creative Commons BY license

RSC Adv., 2021,11, 2359-2376

DNA-encoded libraries (DELs): a review of on-DNA chemistries and their output

Y. Shi, Y. Wu, J. Yu, W. Zhang and C. Zhuang, RSC Adv., 2021, 11, 2359 DOI: 10.1039/D0RA09889B

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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