A kinetic study on the interaction between tazobactam (a penicillanic acid sulphone derivative) and active-site serine beta-lactamases.
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.
Perilli
M
M
Department of Biomedical Sciences and Technologies, University of L'Aquila, Italy.
Franceschini
N
N
Bonfiglio
G
G
Segatore
B
B
Stefani
S
S
Nicoletti
G
G
Perez
M M
MM
Bianchi
C
C
Zollo
A
A
Amicosante
G
G
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
D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D012694:Serine; D010397:Penicillanic Acid; D001618:beta-Lactamases; D000078142:Tazobactam