title: A kinetic study on the interaction between tazobactam (a penicillanic acid sulphone derivative) and active-site serine beta-lactamases.
abstract: The interaction between tazobactam and several chromosome- and plasmid-encoded (TEM, SHV, PSE types) class A and C beta-lactamases was studied by spectrophotometry. Tazobactam behaved as a competitive inhibitor or inactivator able to restore in several cases the efficiency of piperacillin as a partner beta-lactam. A detailed kinetic analysis permitted measurement of the acylation efficiency for some cephalosporinases and broad-spectrum beta-lactamases; the presence of a turn-over of acyl-enzyme complex was also evaluated.
authors.affiliation: Department of Biomedical Sciences and Technologies, University of L'Aquila, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Perilli
authors.forename: N
authors.initials: N
authors.lastname: Franceschini
authors.forename: G
authors.initials: G
authors.lastname: Bonfiglio
authors.forename: B
authors.initials: B
authors.lastname: Segatore
authors.forename: S
authors.initials: S
authors.lastname: Stefani
authors.forename: G
authors.initials: G
authors.lastname: Nicoletti
authors.forename: M M
authors.initials: MM
authors.lastname: Perez
authors.forename: C
authors.initials: C
authors.lastname: Bianchi
authors.forename: A
authors.initials: A
authors.lastname: Zollo
authors.forename: G
authors.initials: G
authors.lastname: Amicosante
mesh_terms: D000150:Acinetobacter / Q000187:drug effects / Q000201:enzymology; D001665:Binding Sites; D002954:Citrobacter / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D007700:Kinetics; D007711:Klebsiella pneumoniae / Q000187:drug effects / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D020596:Morganella / Q000187:drug effects / Q000201:enzymology; D019907:Mycobacterium fortuitum / Q000187:drug effects / Q000201:enzymology; D010397:Penicillanic Acid / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D011532:Providencia / Q000187:drug effects / Q000201:enzymology; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000201:enzymology; D012694:Serine; D012706:Serratia marcescens / Q000187:drug effects / Q000201:enzymology; D000078142:Tazobactam; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000737:chemistry* / Q000235:genetics
chemical_list: D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D012694:Serine; D010397:Penicillanic Acid; D001618:beta-Lactamases; D000078142:Tazobactam