AntibioticsAntibioticResistanceLevofloxacinEscherichiaType II topoisomerasesQuinolonesMutationsSubunitInhibitMycobacteriumAminoglycosidesEnzyme inhibitorGyrA and gyrBTargetsStreptococcusInduceIsolatesReplicationAntimicrobialInhibits bacterialEffluxFluorescenceOfloxacinResistantGenesDoxorubicinTargetFloxacinComplexesNalidixic acidSystemicFosfomycinSusceptibilityCIPROChromosomesEnzymesSupercoilActivityProteinStrand breaks
Antibiotics19
- Knowledge of the first topoisomerase inhibitors, and their medical potential as anticancer drugs and antibiotics, predates the discovery of the first topoisomerase (Escherichia. (wikipedia.org)
- Currently, topoisomerase inhibitors hold a prominent place among antibiotics and anticancer drugs in active medical use, as inhibitors like doxorubicin (anthracycline, TopII inhibitor), etoposide (TopII inhibitor), ciprofloxaxin (fluoroquinolone, TopII inhibitor), and irinotecan (camptothecin derivative, TopI inhibitor) were all included in the 2019 WHO Model List for Essential Medicines. (wikipedia.org)
- Fluoroquinolone antibiotics target bacterial DNA gyrase, an enzyme which reduces DNA strain during replication. (toku-e.com)
- Seay TM, Peretsman SJ and Dixon PS (1996) Inhibition of human transitional cell carcinoma in vitro proliferation by fluoroquinolone antibiotics. (toku-e.com)
- Now fluoroquinolones are broad spectrum bactericidal antibiotics and ciprofloxacin in particular is widely used. (osmosis.org)
- Safety Announcement [12-20-2018] A U.S. Food and Drug Administration (FDA) review found that fluoroquinolone antibiotics can increase the occurrence of rare but serious events of ruptures or tears in the main artery of the body, called the aorta. (kpaddock.com)
- Fluoroquinolone antibiotics are approved to treat certain bacterial infections and have been used for more than 30 years. (kpaddock.com)
- Health care professionals should avoid prescribing fluoroquinolone antibiotics to patients who have an aortic aneurysm or are at risk for an aortic aneurysm, such as patients with peripheral atherosclerotic vascular diseases, hypertension, certain genetic conditions such as Marfan syndrome and Ehlers-Danlos syndrome, and elderly patients. (kpaddock.com)
- Fluoroquinolones (FQs) were introduced as broad-spectrum antibiotics. (biomedcentral.com)
- The response to local changes induced by fluoroquinolone antibiotics, which target DNA gyrase subunit A and/or topoisomerase IV, involves an increase in oxygen radicals which reduces cell viability, while the induction of global supercoiling changes by novobiocin (a DNA gyrase subunit B inhibitor), or by seconeolitsine (a topoisomerase I inhibitor), has revealed the existence of topological domains that specifically respond to such changes. (ucm.es)
- The most effective antibiotics for CBP are fluoroquinolones. (medscape.com)
- Recoveries ranged from The spiked recoveries and relative standard deviations RSDs were Stevens Johnson Syndrome May Be Side Effect of Maxaquin Fluoroquinolones, or quinolones, are a popular group of antibiotics that are some of the most widely prescribed drugs in the nation. (buyotcantibiotics.com)
- Undoing this supercoiling is essential for a bacteria's ability to replicate, so DNA gyrase is a useful target for antibiotics. (tajgenerics.com)
- Fluoroquinolones are a group of broad-spectrum antibiotics that inhibit DNA synthesis. (goldbio.com)
- These antibiotics prevent unwinding of double-stranded DNA by binding DNA gyrase or DNA topoisomerase. (goldbio.com)
- Antibiotics are protein synthesis inhibitors that are used to treat bacterial infections. (buynoprescriptionrxxonline.com)
- Cipro, also known as ciprofloxacin, is an antibiotic that belongs to the fluoroquinolone group of antibiotics. (buynoprescriptionrxxonline.com)
- This study aimed to assay the prevalence of common β-lactam resistance genes including bla TEM , bla SHV , bla CTX-M and bla CMY and phenotypic resistance to commonly used β-lactam and fluoroquinolone antibiotics in UTIs. (biomedcentral.com)
- Several antibiotics are considered for treatment of cystitis and pyelonephritis, including oral β-lactams (amoxicillin-clavulanic acid or third-generation cephalosporin), fluoroquinolones (ciprofloxacin or levofloxacin), nitrofurantoin, fosfomycin or trimethoprim-sulfamethoxazole [ 5 ]. (biomedcentral.com)
Antibiotic8
- Studies searching for antibiotic and anticancer agents in the mid to late 20th century have illuminated the existence of numerous unique families of both TopI and TopII inhibitors, with the 1960s alone resulting in the discovery of the camptothecin, anthracycline and epipodophyllotoxin classes. (wikipedia.org)
- detailed the discovery of the bacterial TopII DNA gyrase and discussed its inhibition when introduced to coumarin and quinolone class inhibitors, sparking greater interest in topoisomerase-targeting antibiotic and antitumor agents. (wikipedia.org)
- Ofloxacin is a synthetic, broad-spectrum, second-generation fluoroquinolone antibiotic that is an analog of nalidixic acid. (toku-e.com)
- The purpose of the study is to discuss the correlation between the resistance rate of gram negative bacteria to fluoroquinolones (FQ) and antibiotic consumption intensity of 145 China tertiary hospitals in 2014. (biomedcentral.com)
- Then the correlation between antibiotic usage and fluoroquinolones -resistant (FQR) rate was consequently investigated. (biomedcentral.com)
- Perfloxacin is a fluoroquinolone antibiotic and is an analog of norfloxacin. (goldbio.com)
- The efficacy of Cipro, a fluoroquinolone antibiotic, has been extensively researched and clinically proven. (buynoprescriptionrxxonline.com)
- This study's results confirmed an explosion of antibiotic resistance amongst E. coli isolates from UTI against β-lactams and fluoroquinolones. (biomedcentral.com)
Resistance14
- Resistance to fluoroquinolones in S . pneu- with MIC 4-8 µg/mL) was caused by a reserpine-sensitive moniae can be acquired by point mutations, intraspecific efflux phenotype (n = 4) or single topoisomerase IV ( parC [n = 24] or parE [n = 1]) changes. (cdc.gov)
- Resistance is caused mainly by amino tance (68 isolates with MIC 16 µg/mL) was caused by acid changes in quinolone resistance-determining regions changes in gyrase ( gyrA ) and parC or parE . (cdc.gov)
- Fluoroquinolones resistance rate varied from hospital to hospital. (biomedcentral.com)
- As this site is distinct from the fluoroquinolone binding site, resistance is not yet documented. (bvsalud.org)
- is impaired by the swift emergence of fluoroquinolone resistance, a trait widely spread among clinical MRSA strains [1, 2]. (pka-inhibitor.com)
- 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. (omicsdi.org)
- This demonstrates that the primary structure of gyrase determines intrinsic quinolone resistance and was supported by a three-dimensional model of N-terminal GyrA. (omicsdi.org)
- To analyze the role of DNA gyrase in quinolone resistance of B. fragilis, we isolated mutant strains by stepwise selection for resistance to increasing concentrations of levofloxacin. (omicsdi.org)
- The gyrA and gyrB sequence information will facilitate analysis of the mechanisms of resistance to drugs which target the gyrase and the implementation of rapid strategies for the estimation of FQ susceptibility in clinical M. tuberculosis isolates. (omicsdi.org)
- DNA gyrase mutations are a major cause of quinolone resistance in Mycobacterium tuberculosis We therefore conducted the first comprehensive study to determine the diversity of gyrase mutations in pre-extensively drug-resistant (pre-XDR) (n = 71) and extensively drug-resistant (XDR) (n = 30) Thai clinical tuberculosis (TB) isolates. (omicsdi.org)
- For 26 EAEC strains highly resistant to fluoroquinolone, minimal inhibitory concentrations for fluoroquinolones were determined, mutations in the quinolone target genes were identified by PCR and sequencing, the presence of transferable quinolone resistance mechanism were identified by PCR, and the contribution of the efflux pump was determined by synergy tests using a proton pump inhibitor. (ophrp.org)
- Increased susceptibility of all the tested isolates to ciprofloxacin and norfloxacin in the presence of the pump inhibitor implies that efflux pumps contributed to the resistance against fluoroquinolones. (ophrp.org)
- Both autophagy inhibitor chloroquine and extracellular vesicles (EVs) release inhibitor GW4869 enhanced doxorubicin activity and counteracted doxorubicin resistance. (preprints.org)
- Phenotypic resistance against β-lactams (ceftazidime, cefotaxime, aztreonam and ceftriaxone) and fluoroquinolones (ciprofloxacin) were identified by the disc diffusion technique. (biomedcentral.com)
Levofloxacin7
- In comparison with findings from the 2002 study, quinolones, such as ciprofloxacin and levofloxacin, topo IV clones Spain14-ST17, Spain23F-ST81, and ST8819F de- and gyrase are primary and secondary targets, respectively creased and 4 new genotypes (ST9710A, ST57016, ST43322, ( 9-13 ). (cdc.gov)
- We demonstrated that Escherichia coli cells exposed to levofloxacin (LVFX), a fluoroquinolone (FQ), induce the syntheses of heat shock proteins and RecA. (biomedcentral.com)
- Levofloxacin is a fluoroquinolone antibacterial indicated in adults (18 years of age and older) with infections caused by designated, susceptible bacteria and in pediatric patients where indicated (1, 12.4). (nih.gov)
- As a fluoroquinolone antibacterial agent, levofloxacin inhibits bacterial type II topoisomerases-DNA gyrase and topoisomerase IV. (medico-labs.com)
- Levofloxacin preferentially targets DNA gyrase in Gram-negative bacteria and topoisomerase IV in Gram-positive bacteria. (medico-labs.com)
- Tendon inflammation and rupture may occur with systemic fluoroquinolone therapy including levofloxacin, particularly in older patients and those treated concurrently with corticosteroids. (medico-labs.com)
- Third-line therapy for Helicobacter pylori infection: Levofloxacin-based Triple Therapy: Levofloxacin, in combination with other antimicrobial agent and proton-pump inhibitor as triple therapy, is indicated for the treatment of patients with gastric ulcer caused by Helicobacter pylori infection and doudenal ulcer disease. (infectweb.com)
Escherichia3
- This series was evaluated in vitro against Escherichia coli DNA gyrase and E. coli topoisomerase IV with the most potent compounds exhibiting IC50 values towards the low micromolar range for DNA gyrase and only â ¼2-fold less active against topoisomerase IV. (bvsalud.org)
- The replacement of M74 in GyrA, A83 in GyrA, and R447 in GyrB of Mycobacterium tuberculosis gyrase by their Escherichia coli homologs resulted in active enzymes as quinolone susceptible as the E. coli gyrase. (omicsdi.org)
- Ulifloxacin is generally more active in vitro than other fluoroquinolones against a variety of clinical isolates of Gram-negative bacteria, including community and nosocomial isolates of Escherichia coli, Klebsiella spp. (ncats.io)
Type II topoisomerases1
- Topoisomerase inhibitors are chemical compounds that block the action of topoisomerases, which are broken into two broad subtypes: type I topoisomerases (TopI) and type II topoisomerases (TopII). (wikipedia.org)
Quinolones5
- There are plenty of processes and enzymes involved that we can target and the quinolones and fluoroquinolones inhibit an enzyme called DNA topoisomerase. (osmosis.org)
- Now, quinolones are created to target bacterial topoisomerases, but it was soon discovered that by adding a fluorine molecule to the quinolones, they become more effective. (osmosis.org)
- So these newer medications, called fluoroquinolones, replaced the older quinolones in most clinical settings. (osmosis.org)
- The quinolones are also known as gyrase inhibitors and are divided into four generations in medicine. (healthandmedicineinfo.com)
- These results suggest that DNA gyrase is an important target for quinolones in B. fragilis. (omicsdi.org)
Mutations1
- Cloning and nucleotide sequence of the DNA gyrase gyrA gene from Serratia marcescens and characterization of mutations in gyrA of quinolone-resistant clinical isolates. (omicsdi.org)
Subunit1
- Molecular docking and simulation studies of the compounds at putative bacterial target enzymes suggest that the antimicrobial potency of these synthesized analogues could be due to enzyme inhibition via their favorable binding at the fluoroquinolone binding site at the GyrA subunit of DNA gyrase and/or the ParC subunit of topoisomerase-IV. (abo.fi)
Inhibit2
- Fluoroquinolones inhibit the activity of DNA gyrase, a type of topoisomerase found in prokaryotes, which prevents a harmful DNA modification called supercoiling. (tajgenerics.com)
- By preventing the formation of single-stranded DNA, fluoroquinolones inhibit bacterial replication. (goldbio.com)
Mycobacterium1
- The emergence of multidrug-resistant strains of Mycobacterium tuberculosis has resulted in increased interest in the fluoroquinolones (FQs) as antituberculosis agents. (omicsdi.org)
Aminoglycosides1
- Treatment of cellulitis caused by uncommon organisms, such as Vibrio species or gram-negative bacteria, should be individualized (eg, tetracyclines, fluoroquinolones or aminoglycosides for Vibrio infection). (medscape.com)
Enzyme inhibitor2
- Long-term beneficial effects of angiotensin-converting enzyme inhibitor and angiotensin receptor blocker therapy for patients with advanced immunoglobulin A nephropathy and impaired renal function. (dnapk-signaling.com)
- An antineoplastic enzyme inhibitor used to treat metastatic carcinoma of the colon or rectum. (drugbank.com)
GyrA and gyrB1
- Molecular cloning of the gyrA and gyrB genes of Bacteroides fragilis encoding DNA gyrase. (omicsdi.org)
Targets3
- One of these targets is bacterial DNA, and we call these medications DNA inhibitors or nucleic acid inhibitors. (osmosis.org)
- One area of research focus is the study of DNA topoisomerases, which are well-established, clinically-validated targets of several anti-cancer agents. (hopkinsmedicine.org)
- Dr. Berger's team has solved structures of topoisomerase targets in complex with target DNA substrates and various drugs. (hopkinsmedicine.org)
Streptococcus1
- Molecular characterization of clinical Streptococcus pneumoniae isolates with reduced susceptibility to fluoroquinolones emerging in Italy. (ncats.io)
Induce1
- Because of this ability to induce apoptosis, topoisomerase inhibitors have gained interest as therapeutics against infectious and cancerous cells. (wikipedia.org)
Isolates1
- We identified two novel orally active inhibitors, PTC-847 and PTC-672, that exhibit a narrow spectrum of activity against Ng including MDR isolates. (elifesciences.org)
Replication5
- It was developed by Daiichi Seiyaku to be resistant to metabolic oxidation in the liver and inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. (toku-e.com)
- Because DNA gyrase is required during DNA replication, subsequent DNA synthesis and ultimately cell division is inhibited. (toku-e.com)
- The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. (buyotcantibiotics.com)
- Lomefloxacin hydrochloride inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. (medindex.am)
- It works by inhibiting the DNA gyrase enzyme, which is essential for bacterial DNA replication. (buynoprescriptionrxxonline.com)
Antimicrobial1
- Clinical use of potentiators have been applied successfully to the antimicrobial class of β-lactams, where β-lactamase inhibitors can significantly enhance the efficacy of β-lactams ( Drawz and Bonomo, 2010 ). (frontiersin.org)
Inhibits bacterial2
- Different emodin derivatives, including the recently reported haloemodin, which inhibits bacterial topoisomerases, can be designed to generate future drugs against resistant pathogens. (longdom.org)
- Inhibits bacterial DNA gyrase (topoisomerase). (enzolifesciences.com)
Efflux1
- However, efflux pumps inhibitors have not yet been approved for treatment of human infections due to tolerability issues ( Fernebro, 2011 ). (frontiersin.org)
Fluorescence1
- Rapid and simultaneous determination of three fluoroquinolones in animal-derived foods using excitation-emission matrix fluorescence coupled with second-order calibration method. (buyotcantibiotics.com)
Ofloxacin2
- Ofloxacin is a Cytochrome P-450 inhibitor and DNA Topoisomerase II inhibitor. (toku-e.com)
- Ofloxacin belongs to the group of fluoroquinolones. (healthandmedicineinfo.com)
Resistant1
- By selecting organisms resistant to the novel inhibitors and sequencing their genomes, we identified a new therapeutic target, the class Ia ribonucleotide reductase (RNR). (elifesciences.org)
Genes2
- The control of DNA-supercoiling in S. pneumoniae occurs mainly via the regulation of topoisomerase gene transcription: relaxation triggers the up-regulation of gyrase and the down-regulation of topoisomerases I and IV, while hypernegative supercoiling down-regulates the expression of topoisomerase I. Relaxation affects 13% of the genome, with the majority of the genes affected located in 15 domains. (ucm.es)
- The genes encoding the DNA gyrase A and B subunits of Bacteroides fragilis were cloned and sequenced. (omicsdi.org)
Doxorubicin1
- Topoisomerase inhibitor classes have been derived from a wide variety of disparate sources, with some being natural products first extracted from plants (camptothecin, etoposide) or bacterial samples (doxorubicin, indolocarbazole), while others possess purely synthetic, and often accidental, origins (quinolone, indenoisoquinoline). (wikipedia.org)
Target4
- However, gyrase is the primary target for moxi- and ST71733) appeared in 2006. (cdc.gov)
- The discovery of an allosteric binding site on the established antibacterial target DNA gyrase offers a new medicinal chemistry strategy. (bvsalud.org)
- DNA gyrase is the main target of the FQs. (omicsdi.org)
- Dr. Berger has a twenty year history of studying the fundamental mechanisms of enzymes that control cell proliferation and small molecule inhibitors that target such systems. (hopkinsmedicine.org)
Floxacin1
- One way to tell a fluoroquinolone apart from other antimicrobials is that they all have the suffix "-floxacin. (osmosis.org)
Complexes2
- Some topoisomerase inhibitors prevent topoisomerases from performing DNA strand breaks while others, deemed topoisomerase poisons, associate with topoisomerase-DNA complexes and prevent the re-ligation step of the topoisomerase mechanism. (wikipedia.org)
- These topoisomerase-DNA-inhibitor complexes are cytotoxic agents, as the un-repaired single- and double stranded DNA breaks they cause can lead to apoptosis and cell death. (wikipedia.org)
Nalidixic acid1
- Topoisomerase inhibitors have been used as important experimental tools that have contributed to the discovery of some topoisomerases, as the quinolone nalidixic acid helped elucidate the bacterial TopII proteins it binds to. (wikipedia.org)
Systemic3
- They can occur with fluoroquinolones for systemic use given by mouth or through an injection. (kpaddock.com)
- Without treatment, some infections can spread and lead to serious health problems (see List of Currently Available FDA-Approved Systemic Fluoroquinolones). (kpaddock.com)
- Systemic fluoroquinolones have been associated with hypersensitivity reactions, even following a single dose. (medico-labs.com)
Fosfomycin1
- Synergistic effect of fosfomycin and fluoroquinolones against Pseudomonas aeruginosa growing in a biofilm. (ncats.io)
Susceptibility1
- The increased susceptibility of the lon mutant was corroborated by experiments in which the gene encoding the cell division inhibitor, SulA, was subsequently disrupted. (biomedcentral.com)
CIPRO2
- Fluoroquinolones, including CIPRO XR, may exacerbate muscle weakness in patients with myasthenia gravis. (globalrph.com)
- Because fluoroquinolones, including CIPRO XR, have been associated with serious adverse reactions [see WARNINGS AND PRECAUTIONS ] and for some patients uncomplicated UTI (acute cystitis) is self-limiting, reserve CIPRO XR for treatment of uncomplicated UTIs (acute cystitis) in patients who have no alternative treatment options. (globalrph.com)
Chromosomes2
- Topoisomerase plays important roles in cellular reproduction and DNA organization, as they mediate the cleavage of single and double stranded DNA to relax supercoils, untangle catenanes, and condense chromosomes in eukaryotic cells. (wikipedia.org)
- Topoisomerase II plays a role in condensing the chromosomes by making a double strand break in the DNA so that it can be more tightly wound, causing a supercoil. (osmosis.org)
Enzymes2
- These are the enzymes topoisomerase II (gyrase) and topoisomerase IV. (healthandmedicineinfo.com)
- After this process, the DNA strand twists again, which requires the two enzymes topoisomerase II and IV. (healthandmedicineinfo.com)
Supercoil1
- DNA-supercoiling is homeostatically maintained by the opposing activities of relaxing DNA topoisomerases and negative supercoil-inducing DNA gyrase. (ucm.es)
Activity2
- Ulifloxacin is a fluoroquinolone with potent antibacterial activity against a broad spectrum of Gram-positive and -negative bacteria. (ncats.io)
- The hydrochloride salt form of lomefloxacin, a synthetic broad-spectrum fluoroquinolone with antibacterial activity. (medindex.am)
Protein1
- It therefore acts as a competitive inhibitor to transpeptidase, an enzyme involved in the cross-linking of peptides, also called penicillin-binding protein. (tajgenerics.com)
Strand breaks2
- Treatment with TopI inhibitors stabilizes the intermediate cleavable complex, preventing DNA re-ligation, and inducing lethal DNA strand breaks. (wikipedia.org)
- Both types of topoisomerases cause double strand breaks in DNA, but at different points during mitosis . (osmosis.org)