| http://purl.uniprot.org/citations/24882105 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/24882105 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/24882105 | http://www.w3.org/2000/01/rdf-schema#comment | "Production of β-lactamases (BLs) is the most widespread resistance mechanism adopted by bacteria to fight β-lactam antibiotics. The substrate spectrum of BLs has become increasingly broad, posing a serious health problem. Thus, there is an urgent need for novel BL inhibitors. Boronic acid transition-state analogues are able to reverse the resistance conferred by class A and C BLs. We describe a boronic acid analogue possessing interesting and potent broad-spectrum activity vs class A and C serine-based BLs. Starting from benzo(b)thiophene-2-boronic acid (BZBTH2B), a nanomolar non-β-lactam inhibitor of AmpC that can potentiate the activity of a third-generation cephalosporin against AmpC-producing resistant bacteria, we designed a novel broad-spectrum nanomolar inhibitor of class A and C BLs. Structure-based drug design (SBDD), synthesis, enzymology data, and X-ray crystallography results are discussed. We clarified the inhibitor binding geometry responsible for broad-spectrum activity vs serine-active BLs using double mutant thermodynamic cycle studies."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm5006572"xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm5006572"xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Shoichet B.K."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Shoichet B.K."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Costi M.P."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Costi M.P."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Venturelli A."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Venturelli A."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Pozzi C."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Pozzi C."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Bonnet R."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Bonnet R."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Tondi D."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/author | "Tondi D."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/date | "2014"xsd:gYear |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/date | "2014"xsd:gYear |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/name | "J. Med. Chem."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/name | "J Med Chem"xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/pages | "5449-5458"xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/pages | "5449-5458"xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/title | "Targeting class A and C serine beta-lactamases with a broad-spectrum boronic acid derivative."xsd:string |
| http://purl.uniprot.org/citations/24882105 | http://purl.uniprot.org/core/title | "Targeting class A and C serine beta-lactamases with a broad-spectrum boronic acid derivative."xsd:string |