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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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Systematic Evolution of Ligands by Exponential Enrichment: RNA Ligands to Bacteriophage T4 DNA Polymerase
Tuerk, C., & Gold, L. (1990) · Science · doi:10.1126/science.2200121 · Cited by 10,421
In vitro selection of RNA molecules that bind specific ligands
Ellington, A. D., & Szostak, J. W. (1990) · Nature · doi:10.1038/346818a0 · Cited by 9,845
Light-Directed, Spatially Addressable Parallel Chemical Synthesis
Fodor, S. P. A., Read, J., Pirrung, M. C., Stryer, L., Lu, A. T., & Solas, D. W. (1991) · Science · doi:10.1126/science.1990438 · Cited by 2,697
Searching for Peptide Ligands with an Epitope Library
Scott, J. K., & Smith, G. P. (1990) · Science · doi:10.1126/science.1696028 · Cited by 2,087
A new type of synthetic peptide library for identifying ligand-binding activity
Lam, K. S., Salmon, S. E., Hersh, E. M., Hruby, V. J., Kazmierski, W. M., & Knapp, R. J. (1991) · Nature · doi:10.1038/354082a0 · Cited by 1,803
Use of peptide synthesis to probe viral antigens for epitopes to a resolution of a single amino acid.
Geysen, H. M., Meloen, R. H., & Barteling, S. J. (1984) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.81.13.3998 · Cited by 1,478
Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery
Houghten, R. A., Pinilla, C., Blondelle, S. E., Appel, J. R., Dooley, C. T., & Cuervo, J. H. (1991) · Nature · doi:10.1038/354084a0 · Cited by 1,327
Peptides on phage: a vast library of peptides for identifying ligands.
Cwirla, S. E., Peters, E. A., Barrett, R. W., & Dower, W. J. (1990) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.87.16.6378 · Cited by 930
CODES WITHOUT COMMAS
Crick, F. H. C., Griffith, J. S., & Orgel, L. E. (1957) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.43.5.416 · Cited by 333

Flagged first, then by citations

Show all 9 references

Research works printed but not linked: 4

[2]Geysen, H. M., Meloen, R. H. & Barteling, S. J. (1984) Proc. Natl. Acad. Sci. USA 81, 3998–4002.
[6]Cwirla, S. E., Peters, E. A., Barrett, R. W. & Dower, W. J. (1990) Proc. Natl. Acad. Sci. USA 87, 6378–6382.
[9]Crick, F. H. C., Griffith, J. S. & Orgel, L. E. (1957) Proc. Natl. Acad. Sci. USA 43, 416–421.
[10]Merrifield, B. (1984) Les Prix Nobel (Almqvist & Wiksell International, Stockholm), pp. 127–153.

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“…process, various encoding methods have been developed to track the synthetic reaction path using either chemical encoding (such as oligonucleotides, 41–43 peptides, 44–46 haloaromatic alcohols, 47–49 dialkylamines 50 ) or non-chemical encoding (such as radiofrequency encoding, 51,52 optical…”
Phagemid Encoded Small Molecules for High Throughput Screening of Chemical Libraries
Yin, J., Liu, F., Schinke, M., Daly, C., & Walsh, C. T. (2004) · Journal of the American Chemical Society · doi:10.1021/ja045127t · Cited by 45
A Small Molecule Selected from a DNA‐Encoded Library of Natural Products That Binds to TNF‐ α and Attenuates Inflammation In Vivo
Wang, S., Shi, X., Li, J., Huang, Q., Ji, Q., Yao, Y., Wang, T., Liu, L., Ye, M., Deng, Y., et al. (2022) · Advanced Science · doi:10.1002/advs.202201258 · Cited by 44
Highly pure DNA-encoded chemical libraries by dual-linker solid-phase synthesis
Keller, M., Petrov, D. D., Gloger, A., Dietschi, B., Jobin, K., Gradinger, T. B., Martinelli, A. L., Plais, L., Onda, Y., Neri, D., et al. (2024) · Science · doi:10.1126/science.adn3412 · Cited by 44
Synthesis of DNA-coupled isoquinolones and pyrrolidines by solid phase ytterbium- and silver-mediated imine chemistry
Potowski, M., Kunig, V. B. K., Losch, F., & Brunschweiger, A. (2019) · MedChemComm · doi:10.1039/c9md00042a · Cited by 45
Developments in Photoredox-Mediated Alkylation for DNA-Encoded Libraries
Patel, S., Badir, S. O., & Molander, G. A. (2020) · Trends in Chemistry · doi:10.1016/j.trechm.2020.11.010 · Cited by 44
Electrochemically Mediated Direct C( sp 3 )−H Sulfonylation of Xanthene Derivatives
Wei, W., Zhong, Y., Feng, Y., Gao, L., Tang, H., Pan, Y., Ma, X., & Mo, Z. (2021) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.202101289 · Cited by 44
An in vitro DNA virus for in vitro protein evolution
Tabuchi, I., Soramoto, S., Nemoto, N., & Husimi, Y. (2001) · FEBS Letters · doi:10.1016/s0014-5793(01)03075-7 · Cited by 44
Modeling protein–ligand interactions for drug discovery in the era of deep learning
Wang, Y. X., Li, Y., Chen, J., & Lai, L. (2025) · Chemical Society Reviews · doi:10.1039/d5cs00415b · Cited by 53
Affinity-based screening techniques: their impact and benefit to increase the number of high quality leads
Bergsdorf, C., & Ottl, J. (2010) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2010.524641 · Cited by 43
“A solidphase synthesis-based approach for such a DNA-encoded combinatorial chemistry screening strategy [9] was further developed by several academic and industry labs for productive ultra-high-throughput affinity screening [10-12].”
Method
Homogeneous and Functional Group Tolerant Ring-Closing Metathesis for DNA-Encoded Chemical Libraries
Monty, O. B. C., Nyshadham, P., Bohren, K. M., Palaniappan, M., Matzuk, M. M., Young, D. W., & Simmons, N. (2020) · ACS Combinatorial Science · doi:10.1021/acscombsci.9b00199 · Cited by 43
Triaging of DNA-Encoded Library Selection Results by High-Throughput Resynthesis of DNA–Conjugate and Affinity Selection Mass Spectrometry
Su, W., Ge, R., Ding, D., Chen, W., Wang, W., Yan, H., Wang, W., Yuan, Y., Liu, H., Zhang, M., et al. (2021) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.1c00170 · Cited by 43
Comparison of Combinatorial Fragment Spaces and Its Application to Ultralarge Make-on-Demand Compound Catalogs
Bellmann, L., Penner, P., Gastreich, M., & Rarey, M. (2022) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.1c01378 · Cited by 43
Solving chemical problems through the application of evolutionary principles
Rozenman, M. M., McNaughton, B. R., & Liu, D. R. (2007) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2007.05.016 · Cited by 43
“Brenner S, Lerner RA: Encoded combinatorial chemistry.”
Background
Unnatural RNA display libraries
Frankel, A., Li, S., Starck, S. R., & Roberts, R. W. (2003) · Current Opinion in Structural Biology · doi:10.1016/s0959-440x(03)00110-6 · Cited by 42
Methods for the Creation of Cyclic Peptide Libraries for Use in Lead Discovery
Foster, A. D., Ingram, J. D., Leitch, E. K., Lennard, K. R., Osher, E. L., & Tavassoli, A. (2015) · SLAS DISCOVERY · doi:10.1177/1087057114566803 · Cited by 42
DNA-encoded chemical libraries of macrocycles
Connors, W. H., Hale, S. P., & Terrett, N. K. (2015) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2015.02.004 · Cited by 41
Hit‐Validation Methodologies for Ligands Isolated from DNA‐Encoded Chemical Libraries
Zimmermann, G., Li, Y., Rieder, U., Mattarella, M., Neri, D., & Scheuermann, J. (2017) · ChemBioChem · doi:10.1002/cbic.201600637 · Cited by 41
Iridium-catalyzed C–H amidation of s -tetrazines
Xiong, H., Gu, Y., Zhang, S., Lu, F., Ji, Q., Liu, L., Ma, P., Yang, G., Hou, W., & Xu, H. (2020) · Chemical Communications · doi:10.1039/d0cc01647k · Cited by 41
Sequential DNA-Encoded Building Block Fusion for the Construction of Polysubstituted Pyrazoline Core Libraries
Zhang, J., Li, X., Wei, H., Li, Y., Zhang, G., & Li, Y. (2021) · Organic Letters · doi:10.1021/acs.orglett.1c03145 · Cited by 41
In-solution direct oxidative coupling for the integration of sulfur/selenium into DNA-encoded chemical libraries
Yang, S., Zhao, G., Gao, Y., Yang, S., Zhang, G., Fan, X., Li, Y., & Li, Y. (2022) · Chemical Science · doi:10.1039/d1sc06268a · Cited by 41
Hybrid Randomised Neighbourhoods Improve Stochastic Local Search for DNA Code Design
Tulpan, D., & Hoos, H. H. (2003) · Lecture notes in computer science · doi:10.1007/3-540-44886-1_31 · Cited by 41
“, sets of DNA strands that satisfy combinatorial constraints, play an important role in various approaches to biomolecular computation [7, 8], nanostructure design [16, 18], and molecular tagging [1, 2, 6].”
BackgroundMethod
Trityl Tags for Encoding in Combinatorial Synthesis
Shchepinov, M. S., Chalk, R., & Southern, E. M. (2000) · Tetrahedron · doi:10.1016/s0040-4020(00)00223-4 · Cited by 41
Simultaneous and combinatorial chemical synthesis techniques for the generation and screening of molecular diversity
Frank, R. (1995) · Journal of Biotechnology · doi:10.1016/0168-1656(95)00062-u · Cited by 41
FASTAptameR 2.0: A web tool for combinatorial sequence selections
Kramer, S. T., Gruenke, P. R., Alam, K. K., Xu, D. H., & Burke, D. H. (2022) · Molecular Therapy — Nucleic Acids · doi:10.1016/j.omtn.2022.08.030 · Cited by 39
“DNA sequence libraries have even been used as barcodes to track lipid nanoparticle formulations and combinatorial chemical synthesis.(22,23) In short, any platform that links polymer sequence (genotype) with a selectable or screenable property (phenotype) can be adapted to combinatorial selections.”
From Concepts to Inhibitors: A Blueprint for Targeting Protein–Protein Interactions
Hong, S. H., Nguyễn, T. T., Ongkingco, J. F., Nazzaro, A., & Arora, P. S. (2025) · Chemical Reviews · doi:10.1021/acs.chemrev.5c00046 · Cited by 45
Selecting a DNA-Encoded Chemical Library against Non-immobilized Proteins Using a “Ligate–Cross-Link–Purify” Strategy
Shi, B., Deng, Y., Zhao, P., & Li, X. (2017) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.7b00343 · Cited by 40
Metal-Catalyzed One-Pot On-DNA Syntheses of Diarylmethane and Thioether Derivatives
Ma, F., Li, J., Zhang, S., Gu, Y., Tan, T., Chen, W., Wang, S., Xu, H., Yang, G., & Lerner, R. A. (2022) · ACS Catalysis · doi:10.1021/acscatal.1c05338 · Cited by 40
Self-citation

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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Encoded combinatorial chemistry.

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