| http://purl.uniprot.org/citations/26731698 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26731698 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26731698 | http://www.w3.org/2000/01/rdf-schema#comment | "Avibactam is a diazabicyclooctane β-lactamase inhibitor possessing outstanding but incomplete efficacy against multidrug-resistant Gram-negative pathogens in combination with β-lactam antibiotics. Significant pharmaceutical investment in generating derivatives of avibactam warrants a thorough characterization of their activity. We show here through structural and kinetic analysis that select diazabicyclooctane derivatives display effective but varied inhibition of two clinically important β-lactamases (CTX-M-15 and OXA-48). Furthermore, these derivatives exhibit considerable antimicrobial activity (MIC ≤ 2 μg/mL) against clinical isolates of Pseudomonas aeruginosa, Escherichia coli, and Enterobacter spp. Imaging of cell phenotype along with structural and biochemical experiments unambiguously demonstrate that this activity, in E. coli, is a result of targeting penicillin-binding protein 2. Our results suggest that structure-activity relationship studies for the purpose of drug discovery must consider both β-lactamases and penicillin-binding proteins as targets. We believe that this approach will yield next-generation combination or monotherapies with an expanded spectrum of activity against currently untreatable Gram-negative pathogens."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.org/dc/terms/identifier | "doi:10.1021/acschembio.5b00944"xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.org/dc/terms/identifier | "doi:10.1021/acschembio.5b00944"xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Wright G.D."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Wright G.D."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Strynadka N.C."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Strynadka N.C."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Brown E.D."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Brown E.D."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "King D.T."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "King D.T."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Parr T.R. Jr."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "King A.M."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "King A.M."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "French S."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "French S."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Vuckovic M."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Vuckovic M."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Malouin F."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Malouin F."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Maiti S.N."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Maiti S.N."xsd:string |
| http://purl.uniprot.org/citations/26731698 | http://purl.uniprot.org/core/author | "Asli A."xsd:string |