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Literature summary for 5.6.2.2 extracted from

  • Gruger, T.; Nitiss, J.L.; Maxwell, A.; Zechiedrich, E.L.; Heisig, P.; Seeber, S.; Pommier, Y.; Strumberg, D.
    A mutation in Escherichia coli DNA gyrase conferring quinolone resistance results in sensitivity to drugs targeting eukaryotic topoisomerase II (2004), Antimicrob. Agents Chemother., 48, 4495-4504.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
DNA sequence determination, mapping and analysis of drug-induced DNA cleavage, expression of wild-type and mutant enzymes in strain JM109 Escherichia coli K-12

Protein Variants

Protein Variants Comment Organism
S83L site-directed mutagenesis, A subunit residue, the mutation leads to enzyme resistance against fluoroquinolones, but increased sensitivity to epipodophyllotoxins and amino-azatoxin in vivo in strain RFM443-242 Escherichia coli K-12
S83W site-directed mutagenesis, A subunit residue, the mutation leads to enzyme resistance against fluoroquinolones, but increased sensitivity to epipodophyllotoxins and amino-azatoxin in vivo in strain RFM443-242 Escherichia coli K-12

Inhibitors

Inhibitors Comment Organism Structure
11beta-(2''-N,N-dimethylaminoethyl)-amino-azatoxin belongs to the epipodophyllotoxins, inhibitors of eukaryotic enzymes, inhibits the S83W mutant enzyme, but not the wild-type bacterial enzyme Escherichia coli K-12
Ciprofloxacin inhibits wild-type enzyme completely at 0.01 mM, 50% inhibition of the mutant S83W at about 0.065 mM Escherichia coli K-12
etoposide belongs to the epipodophyllotoxins, inhibitors of eukaryotic enzymes, inhibits the S83W mutant enzyme, but not the wild-type bacterial enzyme Escherichia coli K-12
fluoroquinolones broad-spectrum antimicrobial agents, Ser83 is responsible for sensitivity, mutation S83W and S83L lead to resistance against the agents Escherichia coli K-12
Teniposide belongs to the epipodophyllotoxins, inhibitors of eukaryotic enzymes, inhibits the S83W mutant enzyme, but not the wild-type bacterial enzyme Escherichia coli K-12

Organism

Organism UniProt Comment Textmining
Escherichia coli K-12
-
 gene gyrA encoding the A subunit
-
Escherichia coli K-12 RFM443
-
 gene gyrA encoding the A subunit
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
 Escherichia coli K-12

Synonyms

Synonyms Comment Organism
DNA gyrase
-
 Escherichia coli K-12
GyrA
-
 Escherichia coli K-12
type II topoisomerase
-
 Escherichia coli K-12