title: Polyphosphate-containing bisubstrate analogues as inhibitors of a bacterial cell wall thymidylyltransferase.
abstract: A series of polyphosphate containing sugar nucleotide analogues were synthesized and evaluated as bisubstrate inhibitors of α-D-glucose 1-phosphate thymidylyltransferase Cps2L, the first enzyme in Streptococcus pneumoniael-rhamnose biosynthesis, and a novel antibacterial target. WaterLOGSY NMR spectroscopy demonstrated binding of bisubstrate analogues to Cps2L and a spectrophotometric coupled assay was used to determine apparent Ki values.
authors: Department of Chemistry, Dalhousie University, 6274 Coburg Rd., PO Box 15, 000, Halifax, Nova Scotia B3H 4R2, Canada. david.jakeman@dal.ca.
authors: Deborah A
authors: DA
authors: Smithen
authors: Stephanie M
authors: SM
authors: Forget
authors: Nicole E
authors: NE
authors: McCormick
authors: Raymond T
authors: RT
authors: Syvitski
authors: David L
authors: DL
authors: Jakeman
mesh_terms: D002473:Cell Wall / Q000187:drug effects* / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009713:Nucleotidyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011122:Polyphosphates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013296:Streptococcus pneumoniae / Q000166:cytology / Q000201:enzymology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011122:Polyphosphates; D009713:Nucleotidyltransferases; C020587:glucose-1-phosphate thymidylyltransferase