Desroy N, Moreau F, Briet S, Fralliec GL, Floquet S, Durant L, Vongsouthi V, Gerusz V, Denis A, Escaich S Towards Gram-negative antivirulence drugs: New inhibitors of HldE kinase Bioorganic and Medicinal Chemistry17(3) (2008)
1276-1289
NCBI PubMed ID:19124251 Journal NLM ID:9413298 Publisher: Elsevier Correspondence: N. Desroy <nicolas.desroymutabilis.fr> Institutions: MUTABILIS SA, 102 Avenue Gaston Roussel, 93230 Romainville, France
Gram-negative bacteria lacking heptoses in their lipopolysaccharide (LPS) display attenuated virulence and increased sensitivity to human serum and to some antibiotics. Thus inhibition of bacterial heptose synthesis represents an attractive target for the development of new antibacterial agents. HldE is a bifunctional enzyme involved in the synthesis of bacterial heptoses. Development of a biochemical assay suitable for high-throughput screening allowed the discovery of inhibitors 1 and 2 of HldE kinase. Study of the structure-activity relationship of this series of inhibitors led to highly potent compounds.
Methods: 1H NMR, ESI-MS, biochemical methods Enzymes that release or process the structure: GmhA, ketose-aldose isomerase Biosynthesis and genetic data: genetic data, biochemical data Synthetic data: chemical
Related record ID(s): 10551, 20419, 23512, 23513 NCBI Taxonomy refs (TaxIDs):562 Reference(s) to other database(s): GTC:G37889CH, GlycomeDB:27767 Show glycosyltransferases
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