ArticleNature chemistry2018
Second-generation DNA-templated macrocycle libraries for the discovery of bioactive small molecules.
Article in Nature chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 79 papers.
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Who cites it
79 citing papers in PubMed.
- Fuel-Driven Catalytic Molecular Templating.Journal of the American Chemical Society · 2026Article
- Massive barcode-free chemical screenings enable the discovery of bioactive macrocycles with passive membrane permeability.Nature communications · 2026Article
- Exploring Size-Controlled Exciton Evolution Using DNA Libraries.Journal of the American Chemical Society · 2026Article
- Enhanced screening via a pure DNA-encoded peptide library enabled by an Fmoc modification.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Aggregation of DNA oligomers with a neutral polymer facilitates DNA solubilization in organic solvents for DNA-encoded chemistry.Chemical science · 2025Article
- Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation.Nature communications · 2025Article
- Enzyme-free biochemical production of seamlessly N-to-C cyclized peptides from natural or recombinant proteins.bioRxiv : the preprint server for biology · 2025Article
- Information propagation through enzyme-free catalytic templating of DNA dimerization with weak product inhibition.Nature chemistry · 2025Article
- Peptide-Oligonucleotide Conjugates: Catalytic Preparation in Aqueous Solution or On-Column.Current protocols · 2025Article
- A Sydnonimine-based Click-and-Release Approach to Cyclic Products.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- A method to identify small molecule/protein pairs susceptible to protein ubiquitination by the CRBN E3 ligase.Chemical science · 2025Article
- Flexibility-tuning of dual-display DNA-encoded chemical libraries facilitates cyclic peptide ligand discovery.Nature communications · 2025Article
- Enzyme-free biochemical production of seamlessly N-to-C cyclized peptides from natural or recombinant proteins.Methods in enzymology · 2025Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Solid-Phase Synthesis of Diverse Macrocycles by Regiospecific 2-Pyridone Formation: Scope and Applications.JACS Au · 2024Article
- Encoding and display technologies for combinatorial libraries in drug discovery: The coming of age from biology to therapy.Acta pharmaceutica Sinica. B · 2024Review
- De novo development of small cyclic peptides that are orally bioavailable.Nature chemical biology · 2024Article
- The motive forces in DNA-enabled nanomachinery.iScience · 2024Review
- Targeted sampling of natural product space to identify bioactive natural product-like polyketide macrolides.Nature communications · 2024Article
- Replication of synthetic recognition-encoded oligomers by ligation of trimer building blocks.Organic chemistry frontiers : an international journal of organic chemistry · 2023Article
19 more citing papers are in PubMed but not listed here.
Corrections and comments
- Erratum issued
Authors and funding
4 authors.
Funding
Abstract
DNA-encoded libraries have emerged as a widely used resource for the discovery of bioactive small molecules, and offer substantial advantages compared with conventional small-molecule libraries. Here, we have developed and streamlined multiple fundamental aspects of DNA-encoded and DNA-templated library synthesis methodology, including computational identification and experimental validation of a 20 × 20 × 20 × 80 set of orthogonal codons, chemical and computational tools for enhancing the structural diversity and drug-likeness of library members, a highly efficient polymerase-mediated template library assembly strategy, and library isolation and purification methods. We have integrated these improved methods to produce a second-generation DNA-templated library of 256,000 small-molecule macrocycles with improved drug-like physical properties. In vitro selection of this library for insulin-degrading enzyme affinity resulted in novel insulin-degrading enzyme inhibitors, including one of unusual potency and novel macrocycle stereochemistry (IC
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.