{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Yang P"],"funding":["Natural Science Foundation of Tianjin City","Ministry of Education of the People&apos;s Republic of China","National Natural Science Foundation of China"],"pagination":["5804-5810"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8179660"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["12(16)"],"pubmed_abstract":["A highly efficient and versatile method for construction of peptide macrocycles <i>via</i> palladium-catalyzed intramolecular <i>S</i>-arylation of alkyl and aryl thiols with aryl iodides under mild conditions is developed. The method exhibits a broad substrate scope for thiols, aryl iodides and amino acid units. Peptide macrocycles of a wide range of size and composition can be readily assembled in high yield from various easily accessible building blocks. This method has been successfully employed to prepare an 8-million-membered tetrameric cyclic peptide DNA-encoded library (DEL). Preliminary screening of the DEL library against protein p300 identified compounds with single digit micromolar inhibition activity."],"journal":["Chemical science"],"pubmed_title":["Streamlined construction of peptide macrocycles <i>via</i> palladium-catalyzed intramolecular <i>S</i>-arylation in solution and on DNA."],"pmcid":["PMC8179660"],"funding_grant_id":["B06005","21877117","21672105","91753124","21725204","18JCZDJC32800","91953203"],"pubmed_authors":["Yang Y","Lu X","He G","Yang P","Chen G","Tong H","Wang X","Li B","Suo Y","Yue J"],"additional_accession":[]},"is_claimable":false,"name":"Streamlined construction of peptide macrocycles <i>via</i> palladium-catalyzed intramolecular <i>S</i>-arylation in solution and on DNA.","description":"A highly efficient and versatile method for construction of peptide macrocycles <i>via</i> palladium-catalyzed intramolecular <i>S</i>-arylation of alkyl and aryl thiols with aryl iodides under mild conditions is developed. The method exhibits a broad substrate scope for thiols, aryl iodides and amino acid units. Peptide macrocycles of a wide range of size and composition can be readily assembled in high yield from various easily accessible building blocks. This method has been successfully employed to prepare an 8-million-membered tetrameric cyclic peptide DNA-encoded library (DEL). Preliminary screening of the DEL library against protein p300 identified compounds with single digit micromolar inhibition activity.","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Mar","modification":"2025-04-04T03:21:06.577Z","creation":"2022-02-10T15:58:36.873Z"},"accession":"S-EPMC8179660","cross_references":{"pubmed":["34168804"],"doi":["10.1039/d1sc00789k"]}}