Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T22348 Target Info
Target Name Bacterial DNA gyrase (Bact gyrase)
Synonyms
DNA gyrase
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Target Type Successful Target
Gene Name Bact gyrA; Bact gyrB
Biochemical Class ATP-hydrolyzing DNA topoisomerase
UniProt ID
GYRA_STAAU; GYRB_STAAU
Co-Targets of This Target  Top
Co-Target Name DNA topoisomerase II beta (TOP2B) Successful Target
UniProt ID TOP2B_HUMAN
Gene Name TOP2B
Synonyms
Topo IIbeta; TOP2beta; TOP2B
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Representative Drug(s) Ciprofloxacin XR Drug Info IC50 = 0.3 ug.mL-1 Click to Show More [1]
2 Ofloxacin Drug Info IC50 = 1 ug.mL-1 [1]
3 Norfloxacin Drug Info Ki = 1 ug ml-1 [2]
Co-Target Name Staphylococcus Topoisomerase IV (Stap-coc parC) Successful Target
UniProt ID PARC_STAAS
Gene Name Stap-coc parC
Synonyms
Topoisomerase IV subunit A; DNA topoisomerase 4 subunit A
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Representative Drug(s) Ciprofloxacin XR Drug Info IC50 = 5 ug.mL-1 Click to Show More [3]
2 Gemifloxacin Drug Info IC50 = 300 nM [5]
Co-Target Name DNA topoisomerase II (TOP2) Successful Target
UniProt ID TOP2A_HUMAN; TOP2B_HUMAN
Gene Name TOP2A; TOP2B
Synonyms
TOP2; DNA topoisomerase 2
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Representative Drug(s) Ciprofloxacin XR Drug Info EC50 = 30 nM [4]
References  Top
REF 1 Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative. J Med Chem. 1988 Sep;31(9):1694-7.
REF 2 Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin). J Med Chem. 1987 Dec;30(12):2283-6.
REF 3 A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus. J Med Chem. 2005 Aug 11;48(16):5232-42.
REF 4 3-benzyl-quinolones: Novel, potent inhibitors of mammalian topoisomerase II. Bioorg Med Chem Lett. 1995 May 4;5(9):1021-6.
REF 5 Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent anti... Bioorg Med Chem Lett. 2006 Mar 1;16(5):1272-6.

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