Tomas Lundqvist

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Glutamate racemase is an enzyme essential to the bacterial cell wall biosynthesis pathway, and has therefore been considered as a target for antibacterial drug discovery. We characterized the glutamate racemases of several pathogenic bacteria using structural and biochemical approaches. Here we describe three distinct mechanisms of regulation for the family(More)
An SAR study of an HTS screening hit generated a series of pyridodiazepine amines as potent inhibitors of Helicobacter pylori glutamate racemase (MurI) showing highly selective anti-H. pylori activity, marked improved solubility, and reduced plasma protein binding. X-ray co-crystal E-I structures were obtained. These uncompetitive inhibitors bind at the(More)
This review comments on some recent trends and insights in the field of lead identification and optimization with a bias toward the increased use of biophysical methods, particularly in combination with three-dimensional structural information. While high-throughput screening, combinatorial chemistry and, most recently, in silico virtual screening(More)
bases (MEDLINE, EMBASE, SCIENCE CITATION INDEX, NHSEED, HEED, CEA REGISTRY, RePEc, HTA database) for manuscripts published between January 2003 and November 2013. Results were assessed for relevance by two reviewers. For eligible studies, data extracted included objectives, costing methodology, sources of data, disaggregated and aggregated costs, and(More)
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