{"doi":"10.1021/jacs.1c12702","title":"Lysine-Targeting Reversible Covalent Inhibitors with Long Residence Time","abstract":"We report a new reversible lysine conjugation that features a novel diazaborine product and much slowed dissociation kinetics in comparison to the previously known iminoboronate chemistry. Incorporating the diazaborine-forming warhead RMR1 to a peptide ligand gives potent and long-acting reversible covalent inhibitors of the staphylococcal sortase. The efficacy of sortase inhibition is demonstrated via biochemical and cell-based assays. A comparative study of RMR1 and an iminoboronate-forming warhead highlights the significance and potential of modulating bond dissociation kinetics in achieving long-acting reversible covalent inhibitors.","journal":"Journal of the American Chemical Society","year":2022,"id":234300,"datarank":0.6980940525236285,"base_score":4.653960350157523,"endowment":4.653960350157523,"self_citation_contribution":0.6980940525236285,"citation_network_contribution":0.0,"self_endowment_contribution":0.6980940525236285,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":104,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9517,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2022-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":289697,"name":"Wenjian Wang","orcid":"0000-0002-1880-3050","position":1,"is_corresponding":false},{"id":850359,"name":"Yuhan Lyu","orcid":null,"position":2,"is_corresponding":false},{"id":850360,"name":"Fredrik Hæffner","orcid":null,"position":3,"is_corresponding":false},{"id":289701,"name":"Jianmin Gao","orcid":"0000-0001-9341-1287","position":4,"is_corresponding":false},{"id":849724,"name":"Rahi M. Reja","orcid":"0000-0001-6219-6326","position":0,"is_corresponding":true}],"reference_count":25,"raw_metadata":{"citation_network_status":"fetched"},"created_at":"2026-07-19T00:21:36.529874Z","pmid":"35040658","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":[]}