{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Antonoplis A"],"funding":["National Cancer Institute","NCI NIH HHS","National Medical Research Council","National Institute of General Medical Sciences","NIGMS NIH HHS","National Science Foundation"],"pagination":["16140-16151"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6430714"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["140(47)"],"pubmed_abstract":["New strategies are urgently needed to target MRSA, a major global health problem and the leading cause of mortality from antibiotic-resistant infections in many countries. Here, we report a general approach to this problem exemplified by the design and synthesis of a vancomycin-d-octaarginine conjugate (V-r8) and investigation of its efficacy in addressing antibiotic-insensitive bacterial populations. V-r8 eradicated MRSA biofilm and persister cells in vitro, outperforming vancomycin by orders of magnitude. It also eliminated 97% of biofilm-associated MRSA in a murine wound infection model and displayed no acute dermal toxicity. This new dual-function conjugate displays enhanced cellular accumulation and membrane perturbation as compared to vancomycin. Based on its rapid and potent activit"],"journal":["Journal of the American Chemical Society"],"pubmed_title":["A Dual-Function Antibiotic-Transporter Conjugate Exhibits Superior Activity in Sterilizing MRSA Biofilms and Killing Persister Cells."],"pmcid":["PMC6430714"],"funding_grant_id":["R01 CA031845","CA031845","NMRC/CBRG/0086/2015","R01 GM117278","R37 CA031845"],"pubmed_authors":["Co JY","Amieva MR","Lee YB","Huttner MA","Kline KA","Zang X","Chong KKL","Cegelski L","Antonoplis A","Wender PA"],"additional_accession":[]},"is_claimable":false,"name":"A Dual-Function Antibiotic-Transporter Conjugate Exhibits Superior Activity in Sterilizing MRSA Biofilms and Killing Persister Cells.","description":"New strategies are urgently needed to target MRSA, a major global health problem and the leading cause of mortality from antibiotic-resistant infections in many countries. Here, we report a general approach to this problem exemplified by the design and synthesis of a vancomycin-d-octaarginine conjugate (V-r8) and investigation of its efficacy in addressing antibiotic-insensitive bacterial populations. V-r8 eradicated MRSA biofilm and persister cells in vitro, outperforming vancomycin by orders of magnitude. It also eliminated 97% of biofilm-associated MRSA in a murine wound infection model and displayed no acute dermal toxicity. This new dual-function conjugate displays enhanced cellular accumulation and membrane perturbation as compared to vancomycin. Based on its rapid and potent activit","dates":{"release":"2018-01-01T00:00:00Z","publication":"2018 Nov","modification":"2025-04-22T04:39:10.992Z","creation":"2019-08-04T07:43:43Z"},"accession":"S-EPMC6430714","cross_references":{"pubmed":["30388366"],"doi":["10.1021/jacs.8b08711"]}}