Cited by 1,014Chemical Synthesis and AnalysisDNA and Nucleic Acid ChemistryClick Chemistry and Applications

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Encoded combinatorial chemistry.

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Brenner, S, Lerner, R A·1992·Proceedings of the National Academy of Sciences

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Abstract

The diversity of chemical synthesis and the power of genetics are linked to provide a powerful, versatile method for drug screening. A process of alternating parallel combinatorial synthesis is used to encode individual members of a large library of chemicals with unique nucleotide sequences. After the chemical entity is bound to a target, the genetic tag can be amplified by replication and utilized for enrichment of the bound molecules by serial hybridization to a subset of the library. The nature of the chemical structure bound to the receptor is decoded by sequencing the nucleotide tag.

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DNA-encoded chemical libraries
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Evolution in vitro: analysis of a lineage of ribozymes
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Photoredox-mediated hydroalkylation and hydroarylation of functionalized olefins for DNA-encoded library synthesis
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Encoded combinatorial chemistry: Synthesis and screening of a library of highly functionalized pyrrolidines
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“Research during these years also brought forth the generation of the ﬁ rst DNA-encoded compound libraries (DECLs) (Brenner & Lerner, 1992; Kinoshita & Nishigaki, 1995) (Fig.”
Background
Navigating large chemical spaces in early-phase drug discovery
Korn, M., Ehrt, C., Ruggiu, F., Gastreich, M., & Rarey, M. (2023) · Current Opinion in Structural Biology · doi:10.1016/j.sbi.2023.102578 · Cited by 71
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Background
Nucleic Acid Templated Reactions for Chemical Biology
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DNA-encoded library versus RNA-encoded library selection enables design of an oncogenic noncoding RNA inhibitor
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“Due to the large number of compounds generated during a combinatorial synthesis, several approaches have been used to identify the structure of the compound carried on an individual bead (2).”
Method
Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S -arylation in solution and on DNA
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Multicomponent Assembly Strategies for the Synthesis of Diverse Tetrahydroisoquinoline Scaffolds
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Phase-trafficking reagents and phase-switching strategies for parallel synthesis
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Multistep DNA-Templated Synthesis Using a Universal Template
Li, Y., Zhao, P., Zhang, M., Zhao, X., & Li, X. (2013) · Journal of the American Chemical Society · doi:10.1021/ja409936r · Cited by 60
Fabrication of Colloidal Crystal Beads by a Drop‐Breaking Technique and Their Application as Bioassays
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Authors: Brenner, S., & Lerner, R. A.
Affiliations: Scripps Research Institute (US)
ORCID: Lerner, R A
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 1992-06-15
Volume: 89
Issue: 12
Pages: 5381-5383
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.89.12.5381
PMC: PMC49295
OpenAlex: W2017423606
Cited by: 1,014
References: 9
Citations by year: 2026: 60 · 2025: 77 · 2024: 71 · 2023: 73 · 2022: 87 · 2021: 72 · 2020: 52 · 2019: 55 · 2018: 30 · 2017: 32 · 2016: 25 · 2015: 24 · 2014: 13 · 2013: 9 · 2012: 8
FWCI: 8.46
Type: journal article
Language: en
Open access: green
europepmc.org
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Topics: Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › DNA and Nucleic Acid Chemistry
Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
Keywords: drug screening, gene tagging, ligand-receptor binding
MeSH terms: Amino Acid Sequence, Base Sequence, Molecular Sequence Data, Peptides, Restriction Mapping, Drug Design, Polymerase Chain Reaction, Databases, Factual

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