ArticleAngewandte Chemie (International ed. in English)2020
TEAD-YAP Interaction Inhibitors and MDM2 Binders from DNA-Encoded Indole-Focused Ugi Peptidomimetics.
Article in Angewandte Chemie (International ed. in English), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed.
- Unleashing the power of DNA-encoded libraries for challenging targets in drug discovery.Pharmaceutical science advances · 2026Review
- Galectin-3 promotes FBXL5-dependent ubiquitination and degradation of YAP1 to constrain colorectal cancer growth.Frontiers in immunology · 2026Article
- Biocatalytic- and Chemoproteomic-Guided Discovery of a PHGDH Inhibitor from Chemoenzymatic-Promoted DNA-Encoded Libraries Selection Platform.Journal of the American Chemical Society · 2025Article
- Aggregation of DNA oligomers with a neutral polymer facilitates DNA solubilization in organic solvents for DNA-encoded chemistry.Chemical science · 2025Article
- RNA-Focused DNA-Encoded Library Construction, Screening, and Integration of Docking Identify Bioactive Ligands of Pathogenic r(GbioRxiv : the preprint server for biology · 2025Article
- Modular Design and Scaffold-Synthesis of Multi-Functional Fluorophores for Targeted Cellular Imaging and Pyroptosis.Angewandte Chemie (International ed. in English) · 2025Article
- FSOACS medicinal chemistry letters · 2024Article
- Combinatorial discovery of antibacterialsChemical science · 2024Article
- Diversifying DNA-Tagged Amines by Isocyanide Multicomponent Reactions for DNA-Encoded Library Synthesis.ACS omega · 2024Article
- Mask and Release Strategy-Enabled Diversity-Oriented Synthesis for DNA-Encoded Library.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Targeting the Hippo/YAP/TAZ signalling pathway: Novel opportunities for therapeutic interventions into skin cancers.Experimental dermatology · 2022Review
- Metal-Free and Open-Air Arylation Reactions of Diaryliodonium Salts for DNA-Encoded Library Synthesis.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- Conjugation of oligonucleotides with activated carbamate reagents prepared by the Ugi reaction for oligonucleotide library synthesis.RSC chemical biology · 2022Article
- Hippo in Gastric Cancer: From Signalling to Therapy.Cancers · 2022Review
- In-solution direct oxidative coupling for the integration of sulfur/selenium into DNA-encoded chemical libraries.Chemical science · 2022Article
- The Hippo pathway in cancer: YAP/TAZ and TEAD as therapeutic targets in cancer.Clinical science (London, England : 1979) · 2022Review
- Discovery of TIGIT inhibitors based on DEL and machine learning.Frontiers in chemistry · 2022Article
- Recent Therapeutic Approaches to Modulate the Hippo Pathway in Oncology and Regenerative Medicine.Cells · 2021Review
- Chemically Stabilized DNA Barcodes for DNA-Encoded Chemistry.Angewandte Chemie (International ed. in English) · 2021Article
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Authors and funding
21 authors.
Funding
Abstract
DNA-encoded combinatorial synthesis provides efficient and dense coverage of chemical space around privileged molecular structures. The indole side chain of tryptophan plays a prominent role in key, or "hot spot", regions of protein-protein interactions. A DNA-encoded combinatorial peptoid library was designed based on the Ugi four-component reaction by employing tryptophan-mimetic indole side chains to probe the surface of target proteins. Several peptoids were synthesized on a chemically stable hexathymidine adapter oligonucleotide "hexT", encoded by DNA sequences, and substituted by azide-alkyne cycloaddition to yield a library of 8112 molecules. Selection experiments for the tumor-relevant proteins MDM2 and TEAD4 yielded MDM2 binders and a novel class of TEAD-YAP interaction inhibitors that perturbed the expression of a gene under the control of these Hippo pathway effectors.
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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.