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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Osawa, T., & Obika, S. (2024) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c23-00295 · Cited by 4
Bioinspired Selenium‐Nitrogen Exchange (SeNEx) Click Chemistry Suitable for Nanomole‐Scale Medicinal Chemistry and Bioconjugation
Hou, W., Zhang, Y., Huang, F., Chen, W., Gu, Y., Wang, Y., Pang, J., Dong, H., Pan, K., Zhang, S., et al. (2024) · Angewandte Chemie · doi:10.1002/ange.202318534 · Cited by 3
Reversible and Fully Controllable Generation of Organo-Soluble DNA (osDNA)
Kumar, S. V., Sunkari, Y. K., Ma, F., Nguyen, T.-L., & Flajolet, M. (2024) · ACS Omega · doi:10.1021/acsomega.3c06755 · Cited by 3
“19,20 A DEL is a mixture of large numbers (millions to billions) of drug-like molecules of small molecular weight, where each molecule is conjugated to a specific and unique DNA-barcode that encodes its chemical structure.”
Background
Optimization of Reaction Conditions for On‐DNA Synthesis of Ureas, Thioureas, and Sulfonamides
Migliorini, F., Ciamarone, A., Neri, D., Cazzamalli, S., & Favalli, N. (2024) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.202400556 · Cited by 3
On‐DNA Transfer Hydrogenolysis and Hydrogenation for the Synthesis of DNA‐Encoded Chemical Libraries
Stanway‐Gordon, H. A., Graham, J. S., & Waring, M. J. (2021) · Angewandte Chemie · doi:10.1002/ange.202111927 · Cited by 3
Synthetic oligonucleotide combinatorial libraries and their applications
Markiewicz, W. T., Astriab, A., Godzina, P., & Markiewicz, M. (2000) · Il Farmaco · doi:10.1016/s0014-827x(00)00014-8 · Cited by 3
Directed evolution of light-activated drugs
Hall, K. D. (1999) · Medical Hypotheses · doi:10.1054/mehy.1999.0799 · Cited by 3
Deterministic Polynomial-Time Algorithms for Designing Short DNA Words
Kao, M., Leung, H. C. M., Sun, H., & Zhang, Y. (2010) · Lecture notes in computer science · doi:10.1007/978-3-642-13562-0_28 · Cited by 3
Combinatorial Chemistry and Multiple Parallel Synthesis
Mitscher, L. A., Aubé, J., Dutta, A., & Golden, J. E. (2010) · Wiley eBooks · doi:10.1002/0471266949.bmc019.pub2 · Cited by 3
Chapter 4 Evolutionary Design of a Model of Self-Assembling Chemical Structures
Buchanan, A., Gazzola, G., & Bedau, M. A. (2008) · Studies in multidisciplinarity · doi:10.1016/s1571-0831(07)00004-4 · Cited by 3
“Combinatorial chemistry [8,12,34] does not employ true evolutionary search.”
Background
Linear Combinatorial Synthesis with Fourier Transform Library Analysis
Schwabacher, A. W., Johnson, C. W., & Geissinger, P. (2003) · Macromolecular Rapid Communications · doi:10.1002/marc.200300157 · Cited by 3
Encoding Strategies for Combinatorial Libraries
Hinzen, B. (2000) · Methods and principles in medicinal chemistry · doi:10.1002/9783527614141.ch05 · Cited by 3
ChemInform Abstract: Molecular Recognition and Solid Phase Organic Synthesis: Synthesis of Unnatural Oligomers, Techniques for Monitoring Reactions, and the Analysis of Combinatorial Libraries
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Oligonucleotide diversity and drug discovery
Trotta, P. P., Beutel, B. A., & Sherman, M. I. (1995) · Medicinal Research Reviews · doi:10.1002/med.2610150403 · Cited by 3
Recent Advances in Chemistry Technologies and Applications to Medicinal Chemistry
Bogdan, A. R., Gesmundo, N. J., Webster, M. P., Wang, Y., & Vasudevan, A. (2021) · Wiley eBooks · doi:10.1002/0471266949.bmc293 · Cited by 3
Orthogonal DNA barcodes enable the high-throughput screening of sequence-defined polymersPreprint
de Rochambeau, D., Hirka, S., Saliba, D., Anderson, S., Toader, V., Dore, M. D., Rizzuto, F. J., McKeague, M., & Sleiman, H. F. (2022) · ChemRxiv · doi:10.26434/chemrxiv-2022-zms0g · Cited by 3
Mass Spectrometry and Drug Discovery
van Breemen, R. B. (2003) · Wiley eBooks · doi:10.1002/0471266949.bmc012 · Cited by 4
Synthetic Combinatorial Libraries: A New Tool for Drug Design
Lebl, M., Krchňák, V., SEPETOV, N. F., Nikolaev, V., Staňková, M., Kočiš, P., Pátek, M., Flegelová, Z., Ferguson, R. D., & Lam, K. S. (1995) · Springer eBooks · doi:10.1007/978-1-4899-1031-8_29 · Cited by 3
On-DNA Binder Confirmation: Increasing Confidence in DEL Hits
Mantell, M. A., Pahil, K. S., Holman, K. R., Alper, J., Jones, C. M., Yao, G., & Marcaurelle, L. A. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01885 · Cited by 3
Unlocking Biomolecule Modification with Light‐Promoted Photocatalyst‐Free Approaches: Current Tools, Challenges, and Perspectives
Hornink, M. M., Thedy, M. E. C., Romero, E., & Molander, G. A. (2025) · ChemistryEurope · doi:10.1002/ceur.202500284 · Cited by 2
On-DNA Deoxygenative C(sp 2 )–C(sp 3 ) Coupling Facilitated by Surfactant–DNA (Surf-DNA) Workflow
Chheda, P. R., Finis, D. S., Simmons, N., & Shi, Z. (2025) · Organic Letters · doi:10.1021/acs.orglett.5c03424 · Cited by 2
Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries
Devakrishnan, A. K., Madasu, C., Wang, Y., Modukuri, R. K., Bohren, K. M., MacKenzie, K. R., Young, D. W., Fuqua, S. A. W., Matzuk, M. M., & Palaniappan, M. (2025) · npj Breast Cancer · doi:10.1038/s41523-025-00837-5 · Cited by 2
“The DNA-encoded library (DEL) platform uses combinatorial chemical synthesis and next-generation DNA sequencing to provide high-throughput, cost-effective af ﬁ nity-based hit discovery 31 – 35 .”

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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