DT-Web

DB04576 - Fleroxacin


Identification
Name Fleroxacin
Accession Number DB04576
Type small molecule
Description Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone. It strongly inhibits the DNA-supercoiling activity of DNA gyrase.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight Not Available
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.
Mechanism of action The inhibition of DNA gyrase and DNA topoisomerase 2 leads ultimately to cell death as these enzymes are required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination.
Absorption Rapidly and well absorbed from the gastrointestinal tract after oral administration.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms Not Available
Interactions
Drug Interactions Not Available
Food Interactions
  • Avoid milk, calcium containing dairy products, iron, magnesium, zinc, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.
  • Avoid excessive coffee or tea (caffeine)
  • Take with a full glass of water
  • Take without regard to meals

Targets


DNA topoisomerase 2-alpha
Name DNA topoisomerase 2-alpha
Gene Name TOP2A
Pharmacological action yes
Actions inhibitor
References
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Robinson MJ, Martin BA, Gootz TD, McGuirk PR, Osheroff N: Effects of novel fluoroquinolones on the catalytic activities of eukaryotic topoisomerase II: Influence of the C-8 fluorine group. Antimicrob Agents Chemother. 1992 Apr;36(4):751-6. - Pubmed
  • Hussy P, Maass G, Tummler B, Grosse F, Schomburg U: Effect of 4-quinolones and novobiocin on calf thymus DNA polymerase alpha primase complex, topoisomerases I and II, and growth of mammalian lymphoblasts. Antimicrob Agents Chemother. 1986 Jun;29(6):1073-8. - Pubmed
DTHybrid score 0.7064
DNA gyrase subunit A
Name DNA gyrase subunit A
Gene Name gyrA
Pharmacological action yes
Actions inhibitor
References
  • Naber KG: Fleroxacin overview. Chemotherapy. 1996 Mar;42 Suppl 1:1-9. - Pubmed
  • Asahina Y, Iwase K, Iinuma F, Hosaka M, Ishizaki T: Synthesis and antibacterial activity of 1-(2-fluorovinyl)-7-substituted-4-quinolone-3-carboxylic acid derivatives, conformationally restricted analogues of fleroxacin. J Med Chem. 2005 May 5;48(9):3194-202. - Pubmed
DTHybrid score 0.9215
DNA topoisomerase 4 subunit A
Name DNA topoisomerase 4 subunit A
Gene Name parC
Pharmacological action yes
Actions inhibitor
References
  • Drlica K, Zhao X: DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. - Pubmed
  • Chaudhry U, Ray K, Bala M, Saluja D: Mutation patterns in gyrA and parC genes of ciprofloxacin resistant isolates of Neisseria gonorrhoeae from India. Sex Transm Infect. 2002 Dec;78(6):440-4. - Pubmed
  • Lee JK, Lee YS, Park YK, Kim BS: Mutations in the gyrA and parC genes in ciprofloxacin-resistant clinical isolates of Acinetobacter baumannii in Korea. Microbiol Immunol. 2005;49(7):647-53. - Pubmed
  • Leavis HL, Willems RJ, Top J, Bonten MJ: High-level ciprofloxacin resistance from point mutations in gyrA and parC confined to global hospital-adapted clonal lineage CC17 of Enterococcus faecium. J Clin Microbiol. 2006 Mar;44(3):1059-64. - Pubmed
DTHybrid score 0.8862

Predictions


Id Partner name Gene Name Score
6224 DNA gyrase subunit A gyrA 0.9215
886 DNA topoisomerase 4 subunit A parC 0.8862
6226 DNA topoisomerase 4 subunit A parC 0.8862
4200 Cytochrome P450 1A2 CYP1A2 0.1722
118 Organic cation/carnitine transporter 2 SLC22A5 0.0949
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0802
1729 Solute carrier family 22 member 6 SLC22A6 0.0761
1588 Multidrug resistance protein 1 ABCB1 0.0703
862 Multidrug resistance-associated protein 1 ABCC1 0.0614
4512 Cytochrome P450 3A4 CYP3A4 0.0549
4192 DNA topoisomerase 2-beta TOP2B 0.044
833 Organic cation/carnitine transporter 1 SLC22A4 0.0392
4118 Cytochrome P450 3A5 CYP3A5 0.0346
4180 DNA-(apurinic or apyrimidinic site) lyase APEX1 0.0305
6144 Solute carrier family 22 member 2 SLC22A2 0.0305
6107 Cytochrome P450 3A7 CYP3A7 0.0282
1353 DNA topoisomerase 1 TOP1 0.0202
3552 DNA topoisomerase 1 topA 0.0202
588 Chromodomain-helicase-DNA-binding protein 1 CHD1 0.0192
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0189
6137 Multidrug resistance-associated protein 6 ABCC6 0.0163
4119 Cytochrome P450 2D6 CYP2D6 0.015
6024 Cytochrome P450 1A1 CYP1A1 0.0147
5718 Cytochrome P450 2A6 CYP2A6 0.0132
2539 Tubulin alpha-1 chain TUBA4A 0.0126
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.012
161 Tubulin beta chain TUBB 0.0117
312 Tubulin beta chain TUB2 0.0117
723 Cytosolic phospholipase A2 PLA2G4A 0.0114
4757 Cytochrome P450 2C9 CYP2C9 0.0112
1898 Cytochrome P450 1B1 CYP1B1 0.0105
6016 Cytochrome P450 2C19 CYP2C19 0.0103
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0089
6148 Multidrug resistance-associated protein 7 ABCC10 0.0075
6013 Cytochrome P450 2E1 CYP2E1 0.0065
992 Protein tyrosine kinase 2 beta PTK2B 0.0064
4120 NADPH--cytochrome P450 reductase POR 0.0053
3947 Xanthine dehydrogenase/oxidase XDH 0.0045
6228 Nuclear receptor coactivator 1 NCOA1 0.0044
6241 Nuclear receptor coactivator 2 NCOA2 0.0043
869 Estrogen receptor beta ESR2 0.0041
776 Bile salt export pump ABCB11 0.0041
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.004
373 Transthyretin TTR 0.0038
6172 ATP-binding cassette sub-family B member 8, mitochondrial ABCB8 0.0036
136 Estrogen receptor ESR1 0.0035
908 Glutathione S-transferase theta-1 GSTT1 0.0032
337 NADH dehydrogenase [ubiquinone] iron-sulfur protein 7, mitochondrial NDUFS7 0.0029
214 NADH dehydrogenase [ubiquinone] iron-sulfur protein 3, mitochondrial NDUFS3 0.0029
803 NADH dehydrogenase [ubiquinone] iron-sulfur protein 2, mitochondrial NDUFS2 0.0029
6168 Solute carrier family 22 member 16 SLC22A16 0.0029
6861 Alcohol dehydrogenase [NADP+] AKR1A1 0.0026
904 Glutathione S-transferase P GSTP1 0.0025
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0023
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0022
650 Aldo-keto reductase family 1 member C3 AKR1C3 0.0021
290 Prostaglandin G/H synthase 2 PTGS2 0.002
20 Prostaglandin G/H synthase 1 PTGS1 0.0019
2157 NAD(P)H dehydrogenase [quinone] 1 NQO1 0.0019
76 Nitric-oxide synthase, brain NOS1 0.0018
4924 Cytochrome P450 2C8 CYP2C8 0.0016
7 Nitric oxide synthase, inducible NOS2 0.0016
291 Nitric-oxide synthase, endothelial NOS3 0.0015
6030 Cytochrome P450 2B6 CYP2B6 0.0012
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