{"doi":"10.1002/asia.202000700","title":"A Macrocyclic Peptide Library with a Structurally Constrained Cyclopropane‐containing Building Block Leads to Thiol‐independent Inhibitors of Phosphoglycerate Mutase","abstract":"Here we report the construction of an mRNA-encoded library of thioether-closed macrocyclic peptides by using an N-chloroacetyl-cyclopropane-containing exotic initiator whose structure is more constrained than the ordinary N-chloroacetyl-α-amino acid initiators. The use of such an initiator has led to a macrocycle library with significantly suppressed population of lariat-shaped species compared with the conventional libraries. We previously used a conventional library and identified a small lariat thioether-macrocycle with a tail peptide with a C-terminal free Cys whose sidechain plays an essential role in potent inhibitory activity against a parasitic model enzyme, phosphoglycerate mutase. On the other hand, the cyclopropane-containing macrocycle library has yielded a larger thioether-macrocycle lacking a free Cys residue, which exhibits potent inhibitory activity to the same enzyme with a different mode of action. This result indicates that such a cyclopropane-containing macrocycle library would allow us to access mechanistically distinct macrocycles.","journal":"Chemistry - An Asian Journal","year":2020,"id":82815,"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":12,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9438,"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":426656,"name":"Tomoki Kuwahara","orcid":"0000-0003-1788-7018","position":1,"is_corresponding":false},{"id":427523,"name":"Takafumi Yoshikane","orcid":null,"position":2,"is_corresponding":false},{"id":426657,"name":"Mizuki Watanabe","orcid":"0000-0001-7209-5713","position":3,"is_corresponding":false},{"id":409319,"name":"Patricia Dranchak","orcid":"0000-0002-1349-4885","position":4,"is_corresponding":false},{"id":409320,"name":"James Inglese","orcid":"0000-0002-7332-5717","position":5,"is_corresponding":false},{"id":426658,"name":"Satoshi Shuto","orcid":"0000-0001-7850-8064","position":6,"is_corresponding":false},{"id":426659,"name":"Yuki Goto","orcid":"0000-0003-4317-0790","position":7,"is_corresponding":false},{"id":426660,"name":"Hiroaki Suga","orcid":"0000-0002-5298-9186","position":8,"is_corresponding":false},{"id":427522,"name":"Rika Okuma","orcid":null,"position":0,"is_corresponding":true}],"reference_count":52,"raw_metadata":null,"created_at":"2026-07-18T21:53:48.608934Z","pmid":"32633882","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":[]}