{"doi":"10.1021/jacs.3c09615","title":"MYC-Targeting Inhibitors Generated from a Stereodiversified Bicyclic Peptide Library","abstract":"High Resolution Image Download MS PowerPoint Slide Here, we present the second generation of our bicyclic peptide library (NTB), featuring a stereodiversified structure and a simplified construction strategy. We utilized a tandem ring-opening metathesis and ring-closing metathesis reaction (ROM-RCM) to cyclize the linear peptide library in a single step, representing the first reported instance of this reaction being applied to the preparation of macrocyclic peptides. Moreover, the resulting bicyclic peptide can be easily linearized for MS/MS sequencing with a one-step deallylation process. We employed this library to screen against the E 363 -R 378 epitope of MYC and identified several MYC-targeting bicyclic peptides. Subsequent in vitro cell studies demonstrated that one candidate, NT-B2R, effectively suppressed MYC transcription activities and cell proliferation.","journal":"Journal of the American Chemical Society","year":2024,"id":422770,"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":25,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9348,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2024-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1217212,"name":"Yi Huang","orcid":"0009-0000-0295-894X","position":1,"is_corresponding":false},{"id":1096966,"name":"Ta I Hung","orcid":"0009-0008-9702-3829","position":2,"is_corresponding":false},{"id":927962,"name":"Jianan Sun","orcid":"0000-0003-4774-6873","position":3,"is_corresponding":false},{"id":879350,"name":"Desiree Aispuro","orcid":null,"position":4,"is_corresponding":false},{"id":878900,"name":"Boxi Chen","orcid":"0009-0001-0702-2558","position":5,"is_corresponding":false},{"id":879351,"name":"Nathan Guevara","orcid":null,"position":6,"is_corresponding":false},{"id":1140011,"name":"Fei Ji","orcid":"0000-0003-1549-3322","position":7,"is_corresponding":false},{"id":1217213,"name":"Cong Xu","orcid":"0000-0002-5426-9721","position":8,"is_corresponding":false},{"id":303372,"name":"Lingchao Zhu","orcid":null,"position":9,"is_corresponding":false},{"id":658863,"name":"Siwen Wang","orcid":"0000-0002-5605-2016","position":10,"is_corresponding":false},{"id":769785,"name":"Zhili Guo","orcid":null,"position":11,"is_corresponding":false},{"id":327109,"name":"Chia‐en A. Chang","orcid":"0000-0002-6504-8529","position":12,"is_corresponding":false},{"id":278771,"name":"Min Xue","orcid":"0000-0002-8136-6551","position":13,"is_corresponding":false},{"id":608861,"name":"Z. Li","orcid":"0000-0002-8362-5617","position":0,"is_corresponding":true}],"reference_count":40,"raw_metadata":null,"created_at":"2026-07-19T01:57:51.642883Z","pmid":"38170904","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":[]}