DNA-Encoded Chemical Libraries: A Comprehensive Review with Succesful Stories and Future Challenges
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Date
2021-08-13
Publication Type
Review Article
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yes
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Abstract
DNA-encoded chemical libraries (DELs) represent a versatile and powerful technology platform for the discovery of small-molecule ligands to protein targets of biological and pharmaceutical interest. DELs are collections of molecules, individually coupled to distinctive DNA tags serving as amplifiable identification barcodes. Thanks to advances in DNA-compatible reactions, selection methodologies, next-generation sequencing, and data analysis, DEL technology allows the construction and screening of libraries of unprecedented size, which has led to the discovery of highly potent ligands, some of which have progressed to clinical trials. In this Review, we present an overview of diverse approaches for the generation and screening of DEL molecular repertoires. Recent success stories are described, detailing how novel ligands were isolated from DEL screening campaigns and were further optimized by medicinal chemistry. The goal of the Review is to capture some of the most recent developments in the field, while also elaborating on future challenges to further improve DEL technology as a therapeutic discovery platform.
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published
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Journal / series
Volume
4 (4)
Pages / Article No.
1265 - 1279
Publisher
American Chemical Society
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Edition / version
Methods
Software
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Date collected
Date created
Subject
DNA-encoded libraries; affinity selections; next-generation sequencing; small molecules; machine learning
Organisational unit
03463 - Neri, Dario (ehemalig) / Neri, Dario (former)
Notes
Funding
163479 - Understanding and Exploiting the Molecular Targeting of Tumor Neo-vasculature (SNF)
670603 - Fulfilling Paul Ehrlich’s Dream: therapeutics with activation on demand (EC)
670603 - Fulfilling Paul Ehrlich’s Dream: therapeutics with activation on demand (EC)