DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information
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The discovery of organic ligands that bind specifically to proteins is a central problem in chemistry, biology, and the biomedical sciences. The encoding of individual organic molecules with distinctive DNA tags, serving as amplifiable identification bar codes, allows the construction and screening of combinatorial libraries of unprecedented size, thus facilitating the discovery of ligands to many different protein targets. Fundamentally, one links powers of genetics and chemical synthesis. After the initial description of DNA-encoded chemical libraries in 1992, several experimental embodiments of the technology have been reduced to practice. This review provides a historical account of important milestones in the development of DNA-encoded chemical libraries, a survey of relevant ongoing research activities, and a glimpse into the future.
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DNA-encoded chemical libraries have made possible synthesis and testing of millions of compounds.
“More recently, DNA-econded chemical libraries have made possible synthesis and testing of millions of compounds165 and many big pharma companies have embraced this approach.”
From QSAR without borders (2020) · cites this paper as [165]
DNA-encoded libraries have the potential to sample vast chemical space (>10^9 compounds) in one or more closely related experiments.
“DNA-encoded libraries (DELs), which have the potential to sample vast chemical space in the span of one or more closely related experiments (>109 compounds) 133 .”
From Targeted protein degradation: expanding the toolbox (2019) · cites this paper as [133]
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Liu, S., Qi, J., Lu, W., Wang, X., & Lu, X. (2021) · Organic Letters · doi:10.1021/acs.orglett.0c04118 · Cited by 45 · see citing works
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Self-citationSynthesis of Multifunctional 2-Aminobenzimidazoles on DNA via Iodine-Promoted Cyclization
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- Authors
- Neri, D., & Lerner, R. A.
- Affiliations
- ETH Zurich (CH)
- Scripps Research Institute (US)
- Venue
- Annual Review of Biochemistry
- Publisher
- Annual Reviews
- Published
- 2018-06-20
- Volume
- 87
- Issue
- 1
- Pages
- 479-502
- ISSN
- 0066-4154 (ISSN-L)
- 1545-4509
- PMC
- PMC6080696
- OpenAlex
- W2782995788
- Cited by
- 364
- References
- 97
- Citations by year
- 2026: 26 · 2025: 32 · 2024: 27 · 2023: 34 · 2022: 42 · 2021: 63 · 2020: 81 · 2019: 46 · 2018: 13
- FWCI
- 5.03
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Annual Review of Biochemistry (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Science Foundation
- Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung (310030B_163479/1, 163479, 160699)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › DNA and Nucleic Acid Chemistry
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Advanced biosensing and bioanalysis techniques
- Keywords
- DNA-encoded libraries, DNA barcoding, combinatorial libraries, protein-ligand binding, ligand discovery, library screening, molecular identification
- MeSH terms
- Animals, Humans, Ligands, Gene Library, Peptide Library, Combinatorial Chemistry Techniques, Small Molecule Libraries, Drug Discovery
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