Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1988-3-11
pubmed:abstractText
The mechanism of action of the quinolone analogs ofloxacin and S-25930, which are unusual because of the presence of a third ring with an asymmetric carbon, was studied. Drug-resistant strains of Escherichia coli were selected by serial passage in the presence of ofloxacin, and a mutation was mapped near the gyrA gene of DNA gyrase. DNA gyrase containing the A subunit purified from this strain as compared with the isogenic wild-type strain exhibited increased resistance to ofloxacin, proving that the mutation was located in the gyrA gene. For S-25930, the S stereoisomer was more potent than the R isomer in inhibiting wild-type E. coli and DNA gyrase containing an A subunit isolated from this strain. Both isomers had decreased potency against the isogenic ofloxacin-resistant (gyrA) strain and its purified enzyme, but the S isomer remained more potent than the R isomer. These studies, using a combined genetic and biochemical approach, demonstrate (i) that DNA gyrase is a target of the tricyclics ofloxacin and S-25930, (ii) that serial exposure to ofloxacin can select resistance to tricyclic quinolone agents by mutation in the gyrA gene, and (iii) that the more potent antibacterial activity of S relative to R S-25930 correlates with increased activity against DNA gyrase for both wild-type and ofloxacin-resistant (gyrA) isogenic strains.
pubmed:grant
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-200930, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-2943589, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3000292, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3010850, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3026239, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3032098, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3034057, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3156025, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-337300, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3460520, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3470281, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3521490, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3532944, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3571042, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3572971, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3864775, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3865923, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-3924878, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-6219620, http://linkedlifedata.com/resource/pubmed/commentcorrection/2829717-6237904
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0066-4804
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1861-3
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Antagonism of wild-type and resistant Escherichia coli and its DNA gyrase by the tricyclic 4-quinolone analogs ofloxacin and S-25930 stereoisomers.
pubmed:affiliation
Medical Services, Massachusetts General Hospital, Boston 02114.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't