Proteins > DNA gyrase subunit B
Page last updated: 2024-08-07 15:50:16
DNA gyrase subunit B
A protein that is a translation product of the gyrB gene in Staphylococcus aureus. [PRO:DNx, UniProtKB:P0A0K8]
Synonyms
EC 5.6.2.2
Research
Bioassay Publications (37)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (8.11) | 29.6817 |
| 2010's | 26 (70.27) | 24.3611 |
| 2020's | 8 (21.62) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| ciprofloxacin | Staphylococcus aureus | IC50 | 57.9980 | 15 | 15 |
| fexofenadine | Staphylococcus aureus | IC50 | 500.0000 | 1 | 1 |
| terfenadine | Staphylococcus aureus | IC50 | 190.0000 | 1 | 1 |
| moxifloxacin | Staphylococcus aureus | IC50 | 14.8017 | 6 | 6 |
| stk295900 | Staphylococcus aureus | IC50 | 0.3000 | 1 | 1 |
| gemifloxacin | Staphylococcus aureus | IC50 | 5.6000 | 4 | 4 |
| ach 702 | Staphylococcus aureus | IC50 | 0.6800 | 1 | 1 |
| ridinilazole | Staphylococcus aureus | IC50 | 50.0000 | 1 | 1 |
| gsk299423 | Staphylococcus aureus | IC50 | 0.0140 | 1 | 1 |
| novobiocin | Staphylococcus aureus | IC50 | 0.0474 | 19 | 19 |
| novobiocin | Staphylococcus aureus | Ki | 0.0360 | 2 | 4 |
| clorobiocin | Staphylococcus aureus | IC50 | 0.0085 | 1 | 1 |
| kibdelomycin | Staphylococcus aureus | IC50 | 0.0090 | 2 | 2 |
| azd0914 | Staphylococcus aureus | IC50 | 4.3000 | 1 | 1 |
| 4-methyl-3-phenyl-1,2-dihydropyrazolo[3,4-b]pyridin-6-one | Staphylococcus aureus | IC50 | 840.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| ciprofloxacin | Staphylococcus aureus | CC50 | 5.0000 | 1 | 1 |
| gatifloxacin | Staphylococcus aureus | CC50 | 0.7000 | 1 | 1 |
| novobiocin | Staphylococcus aureus | MIC | 0.0100 | 1 | 1 |
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors.
Bioorganic & medicinal chemistry letters, , 02-01, Volume: 57, 2022
Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with
Journal of medicinal chemistry, , 10-28, Volume: 64, Issue:20, 2021
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive
ACS medicinal chemistry letters, , Dec-10, Volume: 11, Issue:12, 2020
One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor.
European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
[no title available]
Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety.
Bioorganic & medicinal chemistry letters, , 08-01, Volume: 28, Issue:14, 2018
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity.
Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.
Antimicrobial agents and chemotherapy, , Volume: 54, Issue:7, 2010
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors.
Bioorganic & medicinal chemistry letters, , 02-01, Volume: 57, 2022
Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with
Journal of medicinal chemistry, , 10-28, Volume: 64, Issue:20, 2021
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive
ACS medicinal chemistry letters, , Dec-10, Volume: 11, Issue:12, 2020
One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor.
European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
[no title available]
Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety.
Bioorganic & medicinal chemistry letters, , 08-01, Volume: 28, Issue:14, 2018
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity.
Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.
Antimicrobial agents and chemotherapy, , Volume: 54, Issue:7, 2010
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
The discovery of a novel antibiotic for the treatment of
MedChemComm, , Aug-05, Volume: 6, Issue:8, 2015
MedChemComm, , Aug-05, Volume: 6, Issue:8, 2015
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
The discovery of a novel antibiotic for the treatment of
MedChemComm, , Aug-05, Volume: 6, Issue:8, 2015
MedChemComm, , Aug-05, Volume: 6, Issue:8, 2015
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.
Journal of medicinal chemistry, , 08-22, Volume: 62, Issue:16, 2019
Journal of medicinal chemistry, , 08-22, Volume: 62, Issue:16, 2019
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens.
European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.
ACS medicinal chemistry letters, , Dec-10, Volume: 11, Issue:12, 2020
An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors.
European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
New
MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
[no title available]
Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
New N-phenylpyrrolamide DNA gyrase B inhibitors: Optimization of efficacy and antibacterial activity.
European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors.
European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Linker-switch approach towards new ATP binding site inhibitors of DNA gyrase B.
European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors.
Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
New N-phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATPase inhibitors of DNA gyrase.
European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site.
Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Dual inhibition of Staphylococcus aureus DNA gyrase and topoisomerase IV activity by phenylalanine-derived (Z)-5-arylmethylidene rhodanines.
Bioorganic & medicinal chemistry, , Sep-15, Volume: 23, Issue:18, 2015
Structure-guided design and development of novel benzimidazole class of compounds targeting DNA gyraseB enzyme of Staphylococcus aureus.
Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.
ACS medicinal chemistry letters, , Dec-10, Volume: 11, Issue:12, 2020
An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors.
European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
New
MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
[no title available]
Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
New N-phenylpyrrolamide DNA gyrase B inhibitors: Optimization of efficacy and antibacterial activity.
European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors.
European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Linker-switch approach towards new ATP binding site inhibitors of DNA gyrase B.
European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Discovery of Benzothiazole Scaffold-Based DNA Gyrase B Inhibitors.
Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
New N-phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATPase inhibitors of DNA gyrase.
European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site.
Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Dual inhibition of Staphylococcus aureus DNA gyrase and topoisomerase IV activity by phenylalanine-derived (Z)-5-arylmethylidene rhodanines.
Bioorganic & medicinal chemistry, , Sep-15, Volume: 23, Issue:18, 2015
Structure-guided design and development of novel benzimidazole class of compounds targeting DNA gyraseB enzyme of Staphylococcus aureus.
Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Drug efficacy of novel 3-O-methoxy-4-halo disubstituted 5,7-dimethoxy chromans; evaluated via DNA gyrase inhibition, bacterial cell wall lesion and antibacterial prospective.
Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
New developments in non-quinolone-based antibiotics for the inhibiton of bacterial gyrase and topoisomerase IV.
European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB.
Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016