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