DNA gyrase
DNA gyrase is a bacterial type IIA topoisomerase that controls DNA topology by introducing ATP-dependent negative supercoils into DNA[1]. Mechanistically, this activity supports bacterial genome compaction and resolves topological stress during replication, transcription, and cell division[2]. In E. coli, DNA gyrase functions as an A2B2 heterotetramer, in which GyrA and GyrB form coordinated gates for DNA binding, cleavage, strand passage, and religation[2]. Disease-relevant antibacterial research treats DNA gyrase as a validated target because quinolones stabilize gyrase-DNA cleavage complexes, inhibit DNA synthesis, arrest growth, and can lead to chromosome fragmentation[3]. Compared with topoisomerase IV, DNA gyrase remains especially associated with negative supercoiling, whereas topoisomerase IV also contributes to chromosome unlinking after replication[3]. For experimental applications, quinolones, aminocoumarins, and newer bacterial topoisomerase inhibitors provide mechanistic probes for DNA cleavage, ATPase coupling, conformational intermediates, and resistance-linked target mutations[1][2][3]. - DNA gyrase links bacterial DNA supercoiling control with replication, transcription, chromosome architecture, and antibacterial discovery[1][2]. - GyrA/GyrB organization distinguishes gyrase mechanisms from topoisomerase IV in inhibitor-focused studies[2][3]. - Quinolones and NBTIs support structure-guided analysis of cleavage complexes and resistance mechanisms[2][3].
References:
- [1]. Collin F, et al. Exploiting bacterial DNA gyrase as a drug target: current state and perspectives. Appl Microbiol Biotechnol. 2011;92(3):479-497. [Content Brief]
- [2]. Vanden Broeck A, et al. Cryo-EM structure of the complete E. coli DNA gyrase nucleoprotein complex. Nat Commun. 2019 Oct 30;10(1):4935. [Content Brief]
- [3]. Drlica K, et al. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. [Content Brief]
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DNA gyrase Related Products (6)
Related Products (6)
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DK 507k
0 ImagesCat. No.: HY-107044CAS No.: 364069-14-7DK 507k is an orally active 8-methoxyquinolone Antibacterial agent. DK 507k targets DNA gyrase subunit A (GyrA) and modulates the function of GyrA. DK 507k inhibits the growth of various Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa and Methicillin (HY-121544)-resistant Staphylococcus aureus. DK 507k eliminates Penicillin-tolerant Streptococcus pneumoniae from the lungs of mice. DK 507k can be used in research related to sepsis and *Streptococcus pneumoniae* pneumonia.
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GC-072
0 ImagesCat. No.: HY-178738CAS No.: 1371629-36-5GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis.
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Topoisomerase II-IN-26
0 ImagesCat. No.: HY-184297Topoisomerase II-IN-26 is a dual bacterial type II topoisomerase (Top II) inhibitor, with IC50 values of 0.081 μM and 0.093 μM against Staphylococcus aureus DNA gyrase and topoisomerase IV, respectively, and IC50 values of 0.906 μM and 0.103 μM against Escherichia coli DNA gyrase and topoisomerase IV, respectively. Topoisomerase II-IN-26 also shows high selectivity for human topoisomerase IIα. Topoisomerase II-IN-26 inhibits biofilm formation, reduces the metabolic activity of mature biofilms, exhibits activity against Staphylococcus aureus, MRSA strains, Escherichia coli and Acinetobacter baumannii, and possesses a post-antibiotic effect. Topoisomerase II-IN-26 can be used for the research of bacterial infections such as Staphylococcus aureus and MRSA.
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Antibacterial agent 352
0 ImagesCat. No.: HY-184287Antibacterial agent 352 is an orally active Antibacterial agent. Antibacterial agent 352 binds to the active cavity of Staphylococcus aureus DNA gyrase via hydrogen bonding, π-π stacking and hydrophobic interactions, thereby blocking bacterial DNA synthesis. Antibacterial agent 352 exhibits antibacterial activity against Gram-positive bacteria including Staphylococcus aureus, Bacillus pumilus, Staphylococcus epidermidis and Enterococcus faecalis. Antibacterial agent 352 can disrupt established Staphylococcus aureus biofilms and inhibit the formation of Staphylococcus aureus biofilms. Antibacterial agent 352 can be used in the research of Staphylococcus aureus wound infections.
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Albicidin
0 ImagesCat. No.: HY-108988CAS No.: 1622253-00-2Albicidin is a peptide antibiotic with phytotoxic activity. Albicidin potently inhibits bacterial and plant DNA gyrase at nanomolar concentrations, blocks DNA replication, and exhibits excellent antibacterial efficacy against multidrug-resistant bacteria. Albicidin possesses bactericidal activity against Gram-positive and Gram-negative microorganisms, and acts as a virulence factor for the systemic plant infection by Xanthomonas albilineans. Albicidin can be used in studies related to bacterial infections and sugarcane leaf blight.
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Topoisomerase IV-IN-3
0 ImagesCat. No.: HY-181820Topoisomerase IV-IN-3 is a Staphylococcus aureus Topoisomerase IV inhibitor, DNA gyrase inhibitor and antibacterial agent. Topoisomerase IV-IN-3 has IC50 values of 1.32 μM and 0.48 μM against topoisomerase IV, and 0.88 μM and 0.54 μM against DNA gyrase. Topoisomerase IV-IN-3 inhibits decatenation, ATPase, and supercoiling activities of its target enzymes. Topoisomerase IV-IN-3 exerts antibacterial activity against Gram-positive and Gram-negative bacterial strains. Topoisomerase IV-IN-3 exhibits low cytotoxicity toward human fibroblast cells. Topoisomerase IV-IN-3 can be used for the research of bacterial infections.
