{"doi":"10.17615/4qgg-qe95","title":"Structure–Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains","abstract":"To better understand the contribution of methyl-lysine (Kme) binding proteins to various disease states, we recently developed and reported the discovery of 1 (UNC3866), a chemical probe that targets two families of Kme binding proteins, CBX and CDY chromodomains, with selectivity for CBX4 and -7. The discovery of 1 was enabled in part by the use of molecular dynamics simulations performed with CBX7 and its endogenous substrate. Herein, we describe the design, synthesis and structure-activity relationship studies that led to the development of 1 and provide support for our model of CBX7-ligand recognition by examining the binding kinetics of our antagonists with CBX7 as determined by surface-plasmon resonance.","journal":"INDIGO (University of Illinois at Chicago)","year":2020,"id":142679,"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":0,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9622,"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":392226,"name":"Stephen V. Frye","orcid":"0000-0002-2415-2215","position":1,"is_corresponding":false},{"id":539788,"name":"Nancy Cheng","orcid":null,"position":2,"is_corresponding":false},{"id":395056,"name":"Jacqueline L. Norris‐Drouin","orcid":"0000-0003-1193-4514","position":3,"is_corresponding":false},{"id":609822,"name":"Jacob I. Stuckey","orcid":"0009-0003-1389-5819","position":4,"is_corresponding":false},{"id":541672,"name":"Catherine Simpson","orcid":null,"position":5,"is_corresponding":false},{"id":407308,"name":"Bradley M. Dickson","orcid":"0000-0002-4995-9111","position":6,"is_corresponding":false},{"id":610246,"name":"Ryan Pasca","orcid":null,"position":7,"is_corresponding":false},{"id":396305,"name":"Stephanie H. Cholensky","orcid":null,"position":8,"is_corresponding":false},{"id":540831,"name":"Lindsey I. James","orcid":"0000-0002-6034-7116","position":9,"is_corresponding":false},{"id":609823,"name":"Jung Hyun Lee","orcid":"0000-0002-0496-9826","position":10,"is_corresponding":false},{"id":41818,"name":"Kenneth H. Pearce","orcid":"0000-0001-8138-5421","position":0,"is_corresponding":true}],"reference_count":0,"raw_metadata":null,"created_at":"2026-07-18T23:17:34.768426Z","pmid":null,"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":[]}