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http://purl.uniprot.org/citations/19007108http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/19007108http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/19007108http://www.w3.org/2000/01/rdf-schema#comment"Bacillus anthracis, the causative agent of anthrax, poses a significant biodefense danger. Serious limitations in approved therapeutics and the generation of resistance have produced a compelling need for new therapeutic agents against this organism. Bacillus anthracis is known to be insensitive to the clinically used antifolate, trimethoprim, because of a lack of potency against the dihydrofolate reductase enzyme. Herein, we describe a novel lead series of B. anthracis dihydrofolate reductase inhibitors characterized by an extended trimethoprim-like scaffold. The best lead compound adds only 22 Da to the molecular weight and is 82-fold more potent than trimethoprim. An X-ray crystal structure of this lead compound bound to B. anthracis dihydrofolate reductase in the presence of NADPH was determined to 2.25 A resolution. The structure reveals several features that can be exploited for further development of this lead series."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.org/dc/terms/identifier"doi:10.1021/jm800776a"xsd:string
http://purl.uniprot.org/citations/19007108http://purl.org/dc/terms/identifier"doi:10.1021/jm800776a"xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Anderson A.C."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Anderson A.C."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Wright D.L."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Wright D.L."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Smith A.E."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Smith A.E."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Priestley N.D."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Priestley N.D."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Frey K.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Frey K.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Beierlein J.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Beierlein J.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Bolstad D.B."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Bolstad D.B."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Joska T.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Joska T.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Pelphrey P.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/author"Pelphrey P.M."xsd:string
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/date"2008"xsd:gYear
http://purl.uniprot.org/citations/19007108http://purl.uniprot.org/core/date"2008"xsd:gYear