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

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

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

DOI 10.1038/nrd.2016.213

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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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Authors: Goodnow, R. A., Dumelin, C. E., & Keefe, A. D.
Affiliations: AstraZeneca (United States) (US)
Novartis (Switzerland) (CH)
Corresponding author: Goodnow, Robert A.
ORCID: Goodnow, Robert A.
Dumelin, Christoph E.
Keefe, Anthony D.
Venue: Nature Reviews Drug Discovery
Publisher: Springer Science and Business Media LLC
Published: 2016-12-09
Volume: 16
Issue: 2
Pages: 131-147
ISSN: 1474-1776 (ISSN-L)
1474-1784
DOI: 10.1038/nrd.2016.213
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
Licence: www.springer.com/tdm (tdm)
Locations: Nature Reviews Drug Discovery (publishedVersion)
PubMed (publishedVersion)
Topics: Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › 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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DNA-encoded chemistry: enabling the deeper sampling of chemical space

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