ArticleNature chemistry2023
A DNA-encoded chemical library based on chiral 4-amino-proline enables stereospecific isozyme-selective protein recognition.
Article in Nature chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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16 citing papers in PubMed, 31 citations in OpenAlex.
- From DNA-Encoded Chemistry to Tumor-Targeted Small Molecule Therapeutics.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Integration of palladium-catalyzed C-N coupling into self-encoded libraries for accelerated hit discovery.RSC chemical biology · 2026Article
- Massive barcode-free chemical screenings enable the discovery of bioactive macrocycles with passive membrane permeability.Nature communications · 2026Article
- Toward the Chemoenzymatic Synthesis of DNA-Encoded Libraries.ACS central science · 2026Review
- Discovery of high-affinity ligands for prostatic acid phosphatase via DNA-encoded library screening enables targeted cancer therapy.Nature biomedical engineering · 2026Article
- Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation.Nature communications · 2025Article
- Phenylalanine-Based DNA-Encoded Chemical Libraries for the Discovery of Potent and Selective Small Organic Ligands Against Markers of Cancer and Immune Cells.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Past, present and future of drug conjugates for cancer therapy.Nature cancer · 2025Review
- Visualization of enantiorecognition by excited-state conformation modulation.Nature communications · 2025Article
- Nanopore approaches for single-molecule temporal omics: promises and challenges.Nature methods · 2025Review
- Assembly and biological functions of metal-biomolecule network nanoparticles formed by metal-phosphonate coordination.Science advances · 2024Article
- Covalent DNA-Encoded Library Workflow Drives Discovery of SARS-CoV-2 Nonstructural Protein Inhibitors.Journal of the American Chemical Society · 2024Article
- Translation of Deoxyribonucleic Acid into Synthetic Alpha Helical Peptides for Darwinian Evolution.JACS Au · 2024Article
- FSOACS medicinal chemistry letters · 2024Article
- DNA-encoded chemical libraries enable the discovery of potent PSMA-ligands with substantially reduced affinity towards the GCPIII anti-target.Chemical science · 2024Article
- Impact of library input on the hit discovery rate in DNA-encoded chemical library selections.Chemical science · 2023Article
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Authors and funding
18 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
DNA-encoded chemical libraries (DELs) consist of large chemical compound collections individually linked to DNA barcodes, facilitating pooled construction and screening. However, screening campaigns often fail if the molecular arrangement of the building blocks is not conducive to an efficient interaction with a protein target. Here we postulated that the use of rigid, compact and stereo-defined central scaffolds for DEL synthesis may facilitate the discovery of very specific ligands capable of discriminating between closely related protein targets. We synthesized a DEL comprising 3,735,936 members, featuring the four stereoisomers of 4-aminopyrrolidine-2-carboxylic acid as central scaffolds. The library was screened in comparative selections against pharmaceutically relevant targets and their closely related protein isoforms. Hit validation results revealed a strong impact of stereochemistry, with large affinity differences between stereoisomers. We identified potent isozyme-selective ligands against multiple protein targets. Some of these hits, specific to tumour-associated antigens, demonstrated tumour-selective targeting in vitro and in vivo. Collectively, constructing DELs with stereo-defined elements contributed to high library productivity and ligand selectivity.
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