ArticleACS medicinal chemistry letters2015
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed.
- Covalent DNA-Encoded Library Workflow Drives Discovery of SARS-CoV-2 Nonstructural Protein Inhibitors.Journal of the American Chemical Society · 2024Article
- Osteoarthritis: Insights into Diagnosis, Pathophysiology, Therapeutic Avenues, and the Potential of Natural Extracts.Current issues in molecular biology · 2024Review
- Combining pharmacophore models derived from DNA-encoded chemical libraries with structure-based exploration to predict Tankyrase 1 inhibitors.European journal of medicinal chemistry · 2023Article
- Targeting Aggrecanases for Osteoarthritis Therapy: From Zinc Chelation to Exosite Inhibition.Journal of medicinal chemistry · 2022Review
- Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.ACS medicinal chemistry letters · 2022Article
- Navigating chemical reaction space - application to DNA-encoded chemistry.Chemical science · 2022Article
- Opportunities for Expanding Encoded Chemical Diversification and Improving Hit Enrichment in mRNA-Displayed Peptide Libraries.Chembiochem : a European journal of chemical biology · 2022Review
- DNA-Encoded Chemical Libraries: A Comprehensive Review with Succesful Stories and Future Challenges.ACS pharmacology & translational science · 2021Review
- DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions.Chemical reviews · 2021Review
- Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens.ACS medicinal chemistry letters · 2021Article
- Merging C(spChemical science · 2020Article
- Multifunctional Building Blocks Compatible with Photoredox-Mediated Alkylation for DNA-Encoded Library Synthesis.Organic letters · 2020Article
- A Solution Phase Platform to Characterize Chemical Reaction Compatibility with DNA-Encoded Chemical Library Synthesis.ACS combinatorial science · 2019Article
- Open-Air Alkylation Reactions in Photoredox-Catalyzed DNA-Encoded Library Synthesis.Journal of the American Chemical Society · 2019Article
- Kinetically guided radical-based synthesis of C(spProceedings of the National Academy of Sciences of the United States of America · 2018Article
- Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions.MedChemComm · 2018Article
- DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information.Annual review of biochemistry · 2018Review
- On-DNA Pd and Cu promoted C-N cross-coupling reactions.MedChemComm · 2017Article
- Hit-Validation Methodologies for Ligands Isolated from DNA-Encoded Chemical Libraries.Chembiochem : a European journal of chemical biology · 2017Article
- DNA-encoded chemistry: enabling the deeper sampling of chemical space.Nature reviews. Drug discovery · 2017Review
Corrections and comments
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Authors and funding
14 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The aggrecan degrading metalloprotease ADAMTS-4 has been identified as a novel therapeutic target for osteoarthritis. Here, we use DNA-encoded Library Technology (ELT) to identify novel ADAMTS-4 inhibitors from a DNA-encoded triazine library by affinity selection. Structure-activity relationship studies based on the selection information led to the identification of potent and highly selective inhibitors. For example, 4-(((4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-6-(((4-methylpiperazin-1-yl)methyl)amino)-1,3,5-triazin-2-yl)amino)methyl)-N-ethyl-N-(m-tolyl)benzamide has IC50 of 10 nM against ADAMTS-4, with >1000-fold selectivity over ADAMT-5, MMP-13, TACE, and ADAMTS-13. These inhibitors have no obvious zinc ligand functionality.
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