{"doi":"10.1002/anie.202006280","title":"TEAD–YAP Interaction Inhibitors and MDM2 Binders from DNA‐Encoded Indole‐Focused Ugi Peptidomimetics","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.","journal":"Angewandte Chemie International Edition","year":2020,"id":58323,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":73,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9494,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":306619,"name":"Marco Potowski","orcid":null,"position":1,"is_corresponding":false},{"id":306620,"name":"Mohammad Akbarzadeh","orcid":null,"position":2,"is_corresponding":false},{"id":306621,"name":"Mateja Klika Škopić","orcid":null,"position":3,"is_corresponding":false},{"id":306622,"name":"Denise dos Santos Smith","orcid":null,"position":4,"is_corresponding":false},{"id":306623,"name":"Lukas Arendt","orcid":null,"position":5,"is_corresponding":false},{"id":305441,"name":"Ina Dormuth","orcid":"0000-0003-1921-4917","position":6,"is_corresponding":false},{"id":305442,"name":"Hélène Adihou","orcid":"0000-0003-3005-5259","position":7,"is_corresponding":false},{"id":305443,"name":"Blaž Andlovic","orcid":"0000-0003-0838-3213","position":8,"is_corresponding":false},{"id":305444,"name":"Hacer Karataş","orcid":"0000-0002-7577-0320","position":9,"is_corresponding":false},{"id":305445,"name":"Shabnam Shaabani","orcid":"0000-0001-5546-7140","position":10,"is_corresponding":false},{"id":305446,"name":"Tryfon Zarganes‐Tzitzikas","orcid":"0000-0001-7323-8587","position":11,"is_corresponding":false},{"id":305447,"name":"Constantinos G. Neochoritis","orcid":"0000-0001-5098-5504","position":12,"is_corresponding":false},{"id":305448,"name":"Ran Zhang","orcid":"0000-0001-5160-3491","position":13,"is_corresponding":false},{"id":305449,"name":"Matthew R. Groves","orcid":"0000-0001-9859-5177","position":14,"is_corresponding":false},{"id":305450,"name":"Stéphanie M. Guéret","orcid":"0000-0001-7220-9506","position":15,"is_corresponding":false},{"id":254398,"name":"Christian Ottmann","orcid":"0000-0001-7315-0315","position":16,"is_corresponding":false},{"id":305451,"name":"Jörg Rahnenführer","orcid":"0000-0002-8947-440X","position":17,"is_corresponding":false},{"id":305452,"name":"Roland Fried","orcid":"0000-0002-9830-9713","position":18,"is_corresponding":false},{"id":230785,"name":"Alexander Dömlingꝉ","orcid":"0000-0002-9923-8873","position":19,"is_corresponding":false},{"id":305453,"name":"Andreas Brunschweiger","orcid":"0000-0002-4401-1495","position":20,"is_corresponding":false},{"id":305440,"name":"Verena B. K. Kunig","orcid":"0000-0002-4894-3644","position":0,"is_corresponding":true}],"reference_count":39,"raw_metadata":null,"created_at":"2026-07-18T21:07:11.345501Z","pmid":"32537835","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}