Cited by 644Chemical Synthesis and AnalysisComputational Drug Discovery MethodsDNA and Nucleic Acid Chemistry

DNA-encoded chemistry: enabling the deeper sampling of chemical space

Goodnow, Robert A., Dumelin, Christoph E., Keefe, Anthony D.·2017·Nature Reviews Drug Discovery

Abstract

DNA-encoded chemical library technologies are increasingly being adopted in drug discovery for hit and lead generation. DNA-encoded chemistry enables the exploration of chemical spaces four to five orders of magnitude more deeply than is achievable by traditional high-throughput screening methods. Operation of this technology requires developing a range of capabilities including aqueous synthetic chemistry, building block acquisition, oligonucleotide conjugation, large-scale molecular biological transformations, selection methodologies, PCR, sequencing, sequence data analysis and the analysis of large chemistry spaces. This Review provides an overview of the development and applications of DNA-encoded chemistry, highlighting the challenges and future directions for the use of this technology.

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Crossref · 10.1038/nrd.2016.213

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122 of 122 references verified0 citation errors · 0 not checkable

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  • DELs have allowed screening of drug collections with unprecedented chemical diversity.

    “DELs have allowed the screening of drug collections with an unprecedented chemical diversity.171”

    From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [171]

  • Progress with DELs during the last two decades has transformed this technology into a powerful tool to identify binders.

    “The progress achieved with DELs during the last two decades has transformed this technology into a powerful tool to identify binders.171”

    From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [171]

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Authors
Goodnow, R. A., Dumelin, C. E., & Keefe, A. D.
Affiliations
  • AstraZeneca (United States) (US)
  • Novartis (Switzerland) (CH)
Corresponding author
Goodnow, Robert A.
Venue
Nature Reviews Drug Discovery
Published
2016-12-09
Volume
16
Issue
2
Pages
131-147
ISSN
  • 1474-1776 (ISSN-L)
  • 1474-1784
OpenAlex
W2560677837
Cited by
621
References
122
Citations by year
2026: 52 · 2025: 55 · 2024: 60 · 2023: 51 · 2022: 72 · 2021: 87 · 2020: 85 · 2019: 73 · 2018: 50 · 2017: 36
FWCI
4.83
Type
journal article
Language
en
Open access
closed
Locations
  • Nature Reviews Drug Discovery (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
  • Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › DNA and Nucleic Acid Chemistry
Keywords
DNA-encoded libraries, chemical space exploration, oligonucleotide conjugation, library selection, high-throughput screening, drug discovery
MeSH terms
Animals, Chemistry, DNA, Humans, Genomic Library, Small Molecule Libraries, Drug Discovery, High-Throughput Screening Assays

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