Matches in SemOpenAlex for { <https://semopenalex.org/work/W2972214861> ?p ?o ?g. }
- W2972214861 endingPage "2070" @default.
- W2972214861 startingPage "2065" @default.
- W2972214861 abstract "The emergence of multi-drug-resistant Gram-negative bacteria, including carbapenem-resistant Enterobacteriaceae, is a major health problem that necessitates the development of new antibiotics. Vancomycin inhibits cell-wall synthesis in Gram-positive bacteria but is generally ineffective against Gram-negative bacteria and is unable to penetrate the outer membrane barrier. In an effort to determine whether vancomycin and other antibiotics effective against Gram-positive bacteria could, through modification, be rendered effective against Gram-negative bacteria, we discovered that the covalent attachment of a single arginine to vancomycin yielded conjugates with order-of-magnitude improvements in activity against Gram-negative bacteria, including pathogenic E. coli. The vancomycin–arginine conjugate (V–R) exhibited efficacy against actively growing bacteria, induced the loss of rod cellular morphology, and resulted in the intracellular accumulation of peptidoglycan precursors, all consistent with cell-wall synthesis disruption as its mechanism of action. Membrane permeabilization studies demonstrated an enhanced outer membrane permeability of V–R as compared with vancomycin. The conjugate exhibited no mammalian cell toxicity or hemolytic activity in MTT and hemolysis assays. Our study introduces a new vancomycin derivative effective against Gram-negative bacteria and underscores the broader potential of generating new antibiotics through combined mode-of-action and synthesis-informed design studies." @default.
- W2972214861 created "2019-09-12" @default.
- W2972214861 creator A5022667704 @default.
- W2972214861 creator A5025204479 @default.
- W2972214861 creator A5027151186 @default.
- W2972214861 creator A5037608231 @default.
- W2972214861 creator A5048927292 @default.
- W2972214861 date "2019-09-03" @default.
- W2972214861 modified "2023-10-17" @default.
- W2972214861 title "Vancomycin–Arginine Conjugate Inhibits Growth of Carbapenem-Resistant <i>E. coli</i> and Targets Cell-Wall Synthesis" @default.
- W2972214861 cites W1972775656 @default.
- W2972214861 cites W1979973356 @default.
- W2972214861 cites W1981267913 @default.
- W2972214861 cites W2012251902 @default.
- W2972214861 cites W2020612301 @default.
- W2972214861 cites W2040095685 @default.
- W2972214861 cites W2042143995 @default.
- W2972214861 cites W2056026648 @default.
- W2972214861 cites W2068179698 @default.
- W2972214861 cites W2069449656 @default.
- W2972214861 cites W2076859770 @default.
- W2972214861 cites W2079335891 @default.
- W2972214861 cites W2085065303 @default.
- W2972214861 cites W2102906662 @default.
- W2972214861 cites W2123650819 @default.
- W2972214861 cites W2127206088 @default.
- W2972214861 cites W2150693438 @default.
- W2972214861 cites W2157835441 @default.
- W2972214861 cites W2162322404 @default.
- W2972214861 cites W2165808418 @default.
- W2972214861 cites W2252374742 @default.
- W2972214861 cites W2287479920 @default.
- W2972214861 cites W2288859094 @default.
- W2972214861 cites W2587715799 @default.
- W2972214861 cites W2607111214 @default.
- W2972214861 cites W2613613983 @default.
- W2972214861 cites W2617790881 @default.
- W2972214861 cites W2761317351 @default.
- W2972214861 cites W2790516073 @default.
- W2972214861 cites W2889984933 @default.
- W2972214861 cites W2899315312 @default.
- W2972214861 doi "https://doi.org/10.1021/acschembio.9b00565" @default.
- W2972214861 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6793997" @default.
- W2972214861 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31479234" @default.
- W2972214861 hasPublicationYear "2019" @default.
- W2972214861 type Work @default.
- W2972214861 sameAs 2972214861 @default.
- W2972214861 citedByCount "59" @default.
- W2972214861 countsByYear W29722148612019 @default.
- W2972214861 countsByYear W29722148612020 @default.
- W2972214861 countsByYear W29722148612021 @default.
- W2972214861 countsByYear W29722148612022 @default.
- W2972214861 countsByYear W29722148612023 @default.
- W2972214861 crossrefType "journal-article" @default.
- W2972214861 hasAuthorship W2972214861A5022667704 @default.
- W2972214861 hasAuthorship W2972214861A5025204479 @default.
- W2972214861 hasAuthorship W2972214861A5027151186 @default.
- W2972214861 hasAuthorship W2972214861A5037608231 @default.
- W2972214861 hasAuthorship W2972214861A5048927292 @default.
- W2972214861 hasBestOaLocation W29722148612 @default.
- W2972214861 hasConcept C104317684 @default.
- W2972214861 hasConcept C125235067 @default.
- W2972214861 hasConcept C146587185 @default.
- W2972214861 hasConcept C19655278 @default.
- W2972214861 hasConcept C203014093 @default.
- W2972214861 hasConcept C2776051709 @default.
- W2972214861 hasConcept C2776634448 @default.
- W2972214861 hasConcept C2778980435 @default.
- W2972214861 hasConcept C2779489039 @default.
- W2972214861 hasConcept C2779518903 @default.
- W2972214861 hasConcept C2779902561 @default.
- W2972214861 hasConcept C2992270614 @default.
- W2972214861 hasConcept C3019249092 @default.
- W2972214861 hasConcept C41625074 @default.
- W2972214861 hasConcept C501593827 @default.
- W2972214861 hasConcept C523546767 @default.
- W2972214861 hasConcept C54355233 @default.
- W2972214861 hasConcept C547475151 @default.
- W2972214861 hasConcept C55493867 @default.
- W2972214861 hasConcept C79879829 @default.
- W2972214861 hasConcept C86803240 @default.
- W2972214861 hasConcept C89423630 @default.
- W2972214861 hasConceptScore W2972214861C104317684 @default.
- W2972214861 hasConceptScore W2972214861C125235067 @default.
- W2972214861 hasConceptScore W2972214861C146587185 @default.
- W2972214861 hasConceptScore W2972214861C19655278 @default.
- W2972214861 hasConceptScore W2972214861C203014093 @default.
- W2972214861 hasConceptScore W2972214861C2776051709 @default.
- W2972214861 hasConceptScore W2972214861C2776634448 @default.
- W2972214861 hasConceptScore W2972214861C2778980435 @default.
- W2972214861 hasConceptScore W2972214861C2779489039 @default.
- W2972214861 hasConceptScore W2972214861C2779518903 @default.
- W2972214861 hasConceptScore W2972214861C2779902561 @default.
- W2972214861 hasConceptScore W2972214861C2992270614 @default.
- W2972214861 hasConceptScore W2972214861C3019249092 @default.
- W2972214861 hasConceptScore W2972214861C41625074 @default.
- W2972214861 hasConceptScore W2972214861C501593827 @default.
- W2972214861 hasConceptScore W2972214861C523546767 @default.