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PMID: 6792979 Published · ppublish English Journal Article Research Support, U.S. Gov't, Non-P.H.S.

Competition of beta-lactam antibiotics for the penicillin-binding proteins of Neisseria gonorrhoeae.

Antimicrobial agents and chemotherapy ·Vol. 20 ·No. 1 ·1981-07-00 ·Pages 109-14

Dougherty TJ, Koller AE, Tomasz A

Abstract

The affinities of nine structurally different beta-lactam antibiotics for the three major gonococcal penicillin-binding proteins (PBPs) were determined by using a competition assay with tritium-labeled penicillin and live, growing bacteria. Each determination was carried out in parallel in isogenic pairs of penicillin-susceptible (minimal inhibitory concentration of penicillin, 0.0075 microgram/ml) and intrinsically penicillin-resistant (minimal inhibitory concentration of penicillin, 0.5 microgram/ml) cells. Evidence is presented indicating that (i) PBP 3 may be a dispensable function; (ii) acquisition of resistance is accompanied by change in the beta-lactam antibiotic affinities of PBP 2 but not of PBP 1; (iii) PBP 2 appears to be the most important physiological target in the penicillin-susceptible strain; in the penicillin-resistant strain, PBP 1 seems to assume this role. The relative affinities of various beta-lactam antibiotics for the individual PBPs showed substantial variation with the antibiotic structure.

MeSH Terms
Bacterial Proteins Binding, Competitive Carrier Proteins/metabolism Cephalosporins/metabolism,pharmacology Hexosyltransferases Muramoylpentapeptide Carboxypeptidase Neisseria gonorrhoeae/drug effects,metabolism Penicillin-Binding Proteins Penicillins/metabolism,pharmacology Peptidyl Transferases
Chemicals
Bacterial Proteins Carrier Proteins Cephalosporins Penicillin-Binding Proteins Penicillins Peptidyl Transferases Hexosyltransferases Muramoylpentapeptide Carboxypeptidase
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Dougherty T J
Koller A E
Tomasz A
References (16)
16 references, click to expand
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Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
DOI
10.1128/AAC.20.1.109
Published
1981-07-00
Pages
109-14
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC181641
Subset
IM
External Links
PubMed source DOI: 10.1128/AAC.20.1.109 PMC Full Text View journal details
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