title: Antibacterial drug discovery and structure-based design.
abstract: Bacterial resistance continues to develop and pose a significant threat, both in hospitals and, more recently, in the community. A focus on other therapeutic areas by the larger pharmaceutical companies has left a shortfall in the pipeline of novel antibacterials. Recently, many new structures have been studied by structure-genomics initiatives, delivering a wealth of targets to consider. Using the tools of structure-based design, antibacterial discovery must exploit these targets to accelerate the process of drug discovery.
authors.affiliation: Evotec UK, 111 Milton Park, Abingdon, Oxfordshire, OX14 4RZ, UK. john.barker@evotec.com
authors.forename: John J
authors.initials: JJ
authors.lastname: Barker
mesh_terms: D000081:Acetamides / Q000737:chemistry / Q000494:pharmacology; D000604:Amino Acyl-tRNA Synthetases / Q000037:antagonists & inhibitors / Q000378:metabolism; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects* / Q000201:enzymology; D018360:Crystallography, X-Ray; D004250:DNA Topoisomerases, Type II / Q000737:chemistry / Q000378:metabolism; D015195:Drug Design; D024881:Drug Resistance, Bacterial; D006801:Humans; D000069349:Linezolid; D008958:Models, Molecular; D015394:Molecular Structure; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D023303:Oxazolidinones / Q000737:chemistry / Q000494:pharmacology; D014176:Protein Biosynthesis; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors; D014158:Transcription, Genetic
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D008996:Monoamine Oxidase Inhibitors; D023303:Oxazolidinones; D059005:Topoisomerase II Inhibitors; D004250:DNA Topoisomerases, Type II; D000604:Amino Acyl-tRNA Synthetases; D000069349:Linezolid