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http://purl.uniprot.org/citations/29844038http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/29844038http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/29844038http://www.w3.org/2000/01/rdf-schema#comment"CTX-M is the most prevalent family of extended-spectrum β-lactamases. We recently developed a tetrazole-derived noncovalent inhibitor of CTX-M-9. Here, we present the biochemical and microbiological activity of this inhibitor across a representative panel of serine β-lactamases and Gram-negative bacteria. The compound displayed significant activity against all major subgroups of CTX-M, including CTX-M-15, while it exhibited some low-level inhibition of other serine β-lactamases. Complex crystal structures with the CTX-M-14 S237A mutant and CTX-M-27 illustrate the binding contribution of specific active-site residues on the β3 strand. In vitro pharmacokinetic studies revealed drug-like properties and positive prospects for further optimization. These studies suggest that tetrazole-based compounds can provide novel chemotypes for future serine β-lactamase inhibitor discovery."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.org/dc/terms/identifier"doi:10.1128/aac.02563-17"xsd:string
http://purl.uniprot.org/citations/29844038http://purl.org/dc/terms/identifier"doi:10.1128/aac.02563-17"xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Chen Y."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Chen Y."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Zhang X."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Zhang X."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Adams J."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Adams J."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Shaw L.N."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Shaw L.N."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Jaishankar P."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Jaishankar P."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Renslo A.R."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Renslo A.R."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Bonnet R."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Bonnet R."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"DeFrees K."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"DeFrees K."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Nichols D.A."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Nichols D.A."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Pemberton O.A."xsd:string
http://purl.uniprot.org/citations/29844038http://purl.uniprot.org/core/author"Pemberton O.A."xsd:string