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DNA gyrase subunit A
A DNA gyrase subunit A that is encoded in the genome of Mycobacterium tuberculosis H37Rv. [PRO:DNx]
Synonyms
EC 5.6.2.2;
Type IIA topoisomerase subunit GyrA
Research
Bioassay Publications (19)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (5.26) | 29.6817 |
| 2010's | 17 (89.47) | 24.3611 |
| 2020's | 1 (5.26) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ciprofloxacin | Mycobacterium tuberculosis H37Rv | IC50 | 19.4418 | 3 | 3 |
| enoxacin | Mycobacterium tuberculosis H37Rv | IC50 | 156.0000 | 1 | 1 |
| isoniazid | Mycobacterium tuberculosis H37Rv | IC50 | 50.0000 | 1 | 1 |
| vitamin k 3 | Mycobacterium tuberculosis H37Rv | IC50 | 200.0000 | 2 | 2 |
| nalidixic acid | Mycobacterium tuberculosis H37Rv | IC50 | 4,750.0000 | 1 | 1 |
| ofloxacin | Mycobacterium tuberculosis H37Rv | IC50 | 28.0000 | 1 | 1 |
| gatifloxacin | Mycobacterium tuberculosis H37Rv | IC50 | 27.1333 | 3 | 3 |
| 7-methyljuglone | Mycobacterium tuberculosis H37Rv | IC50 | 30.0000 | 2 | 2 |
| isodiospyrin | Mycobacterium tuberculosis H37Rv | IC50 | 100.0000 | 2 | 2 |
| levofloxacin | Mycobacterium tuberculosis H37Rv | IC50 | 217.3333 | 3 | 3 |
| moxifloxacin | Mycobacterium tuberculosis H37Rv | IC50 | 15.6231 | 13 | 13 |
| diospyrin | Mycobacterium tuberculosis H37Rv | IC50 | 15.0000 | 2 | 2 |
| isoshinanolone | Mycobacterium tuberculosis H37Rv | IC50 | 200.0000 | 1 | 1 |
| stk295900 | Mycobacterium tuberculosis H37Rv | IC50 | 11.3000 | 1 | 1 |
| ach 702 | Mycobacterium tuberculosis H37Rv | IC50 | 5.1333 | 3 | 3 |
| novobiocin | Mycobacterium tuberculosis H37Rv | IC50 | 3.9538 | 12 | 12 |
| azd0914 | Mycobacterium tuberculosis H37Rv | IC50 | 32.0000 | 1 | 1 |
| rifampin | Mycobacterium tuberculosis H37Rv | IC50 | 50.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ofloxacin | Mycobacterium tuberculosis H37Rv | CC25 | 7.0000 | 1 | 1 |
| moxifloxacin | Mycobacterium tuberculosis H37Rv | CC25 | 2.0000 | 1 | 1 |
Design, synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
A novel synthesis of 2-arylbenzimidazoles in molecular sieves-MeOH system and their antitubercular activity.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
The naphthoquinone diospyrin is an inhibitor of DNA gyrase with a novel mechanism of action.The Journal of biological chemistry, , Feb-15, Volume: 288, Issue:7, 2013
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 24, Issue:1, 2016
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
4-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.ACS medicinal chemistry letters, , Jul-09, Volume: 6, Issue:7, 2015
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:8, 2010
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:8, 2008
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 24, Issue:1, 2016
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
4-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.Bioorganic & medicinal chemistry, , Dec-01, Volume: 22, Issue:23, 2014
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Thiazole-aminopiperidine hybrid analogues: design and synthesis of novel Mycobacterium tuberculosis GyrB inhibitors.European journal of medicinal chemistry, , Volume: 70, 2013
The naphthoquinone diospyrin is an inhibitor of DNA gyrase with a novel mechanism of action.The Journal of biological chemistry, , Feb-15, Volume: 288, Issue:7, 2013