{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Reja RM"],"funding":["Division of Chemistry","Ono Pharma Foundation","National Institute of General Medical Sciences","NIGMS NIH HHS","NIH HHS"],"pagination":["1152-1157"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8928449"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["144(3)"],"pubmed_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"],"pubmed_title":["Lysine-Targeting Reversible Covalent Inhibitors with Long Residence Time."],"pmcid":["PMC8928449"],"funding_grant_id":["GM102735","CHE-1904874","R01 GM102735","R01 GM124231","S10 OD026910"],"pubmed_authors":["Haeffner F","Lyu Y","Gao J","Wang W","Reja RM"],"additional_accession":[]},"is_claimable":false,"name":"Lysine-Targeting Reversible Covalent Inhibitors with Long Residence Time.","description":"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.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Jan","modification":"2026-05-09T13:44:43.393Z","creation":"2025-04-07T03:19:38.805Z"},"accession":"S-EPMC8928449","cross_references":{"pubmed":["35040658"],"doi":["10.1021/jacs.1c12702"]}}