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FEBS Lett. 2018 Jun;592(12):2168-2180. doi: 10.1002/1873-3468.13068. Epub 2018 May 10.

DNA-encoded chemical libraries - achievements and remaining challenges.

Author information

1
Department of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology (ETH Zürich), Zürich, Switzerland.

Abstract

DNA-encoded chemical libraries (DECLs) are collections of compounds, individually coupled to DNA tags serving as amplifiable identification barcodes. Since individual compounds can be identified by the associated DNA tag, they can be stored as a mixture, allowing the synthesis and screening of combinatorial libraries of unprecedented size, facilitated by the implementation of split-and-pool synthetic procedures or other experimental methodologies. In this review, we briefly present relevant concepts and technologies, which are required for the implementation and interpretation of screening procedures with DNA-encoded chemical libraries. Moreover, we illustrate some success stories, detailing how novel ligands were discovered from encoded libraries. Finally, we critically review what can realistically be achieved with the technology at the present time, highlighting challenges and opportunities for the future.

KEYWORDS:

DNA ; DNA-encoded chemical libraries; combinatorial chemistry; drug discovery; high-throughput DNA sequencing

PMID:
29683493
PMCID:
PMC6126621
DOI:
10.1002/1873-3468.13068
[Indexed for MEDLINE]
Free PMC Article

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