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PMID: 7574520 Published · ppublish English Comparative Study Journal Article Research Support, Non-U.S. Gov't

Interactions of biapenem with active-site serine and metallo-beta-lactamases.

Antimicrobial agents and chemotherapy ·Vol. 39 ·No. 6 ·1995-06-00 ·Pages 1300-5

Felici A, Perilli M, Segatore B, Franceschini N, Setacci D, Oratore A, Stefani S, Galleni M, Amicosante G

Abstract

Biapenem, formerly LJC 10,627 or L-627, a carbapenem antibiotic, was studied in its interactions with 12 beta-lactamases belonging to the four molecular classes proposed by R. P. Ambler (Philos. Trans. R. Soc. Lond. Biol. Sci. 289:321-331, 1980). Kinetic parameters were determined. Biapenem was readily inactivated by metallo-beta-lactamases but behaved as a transient inhibitor of the active-site serine enzymes tested, although with different acylation efficiency values. Class A and class D beta-lactamases were unable to confer in vitro resistance toward this carbapenem antibiotic. Surprisingly, the same situation was found in the case of class B enzymes from Aeromonas hydrophila AE036 and Bacillus cereus 5/B/6 when expressed in Escherichia coli strains.

MeSH Terms
Binding Sites Enterobacteriaceae/drug effects,enzymology Enzyme Activation Enzyme Inhibitors Imipenem/metabolism,pharmacology Kinetics Metalloproteins/metabolism Microbial Sensitivity Tests Serine/metabolism Thienamycins/metabolism,pharmacology Zinc/metabolism beta-Lactam Resistance beta-Lactamases/classification,drug effects,metabolism
Chemicals
Enzyme Inhibitors Metalloproteins Thienamycins Serine Imipenem beta-Lactamases Zinc biapenem
Authors & Affiliations
9 authors, click to expand affiliations / ORCID
Felici A
Dipartimento di Scienze e Tecnologie Biomediche e di Biometria, Università degli Studi dell'Aquila, Italy.
Perilli M
Segatore B
Franceschini N
Setacci D
Oratore A
Stefani S
Galleni M
Amicosante G
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Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
DOI
10.1128/AAC.39.6.1300
Published
1995-06-00
Pages
1300-5
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC162731
Subset
IM
External Links
PubMed source DOI: 10.1128/AAC.39.6.1300 PMC Full Text View journal details
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