Related Experiment Video
Updated: Aug 6, 2026
10:27
Dual DNA Rulers to Study the Mechanism of Ribosome Translocation with Single-Nucleotide Resolution
Published on: July 8, 2019
Advances in DNA gyrase inhibitors
O K Kim1, K Ohemeng, J F Barrett
1Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA.
Expert Opinion on Investigational Drugs
|February 15, 2001
Summary
New quinolone antibacterials and novel non-fluoroquinolone DNA gyrase inhibitors show improved potency and safety for treating bacterial infections. Ongoing research expands options for novel antibacterial drug development.
Area of Science:
- Microbiology
- Medicinal Chemistry
- Pharmacology
Background:
- DNA gyrase inhibitors, primarily quinolone antibacterials, are vital for treating bacterial infections.
- Recent advancements have introduced new quinolones with enhanced properties.
Purpose of the Study:
- To review recent developments in DNA gyrase inhibitors.
- To highlight novel antibacterial compounds and their potential.
Main Methods:
- Review of recent research and development in quinolone antibacterials.
- Analysis of newly discovered non-fluoroquinolone and 2-pyridone antibacterials.
Main Results:
- New quinolones (moxifloxacin, gatifloxacin, gemifloxacin) demonstrate equal or superior potency, spectrum, pharmacodynamics, pharmacokinetics, and safety.
- Emerging non-fluoroquinolone and 2-pyridone antibacterials offer new chemotypes for DNA gyrase inhibition.
Conclusions:
- Recent quinolone development offers improved therapeutic options.
- Novel antibacterial classes expand the landscape for future DNA gyrase inhibitor discovery and development.
Related Concept Videos
02:27DNA Base Pairing
Erwin Chargaff’s rules on DNA equivalence paved the way for the discovery of base pairing in DNA. Chargaff’s rules state that in a double-stranded DNA molecule,
00:55DNA Helicases
DNA unwinding helicase enzymes are a type of motor protein. Motor proteins can translocate along filaments or polymers using energy generated from ATP hydrolysis. Helicases are involved in all the important cellular processes where DNA unwinding is required, such as DNA replication, repair, recombination, and transcription. They are present in all living organisms, but vary in their structure, function, and mechanism of action. For example, in prokaryotes, DnaB helicase binds and translocates...
01:23Inhibitors of Gram-positive Cell Wall Synthesis
Bacterial cell walls are typically rigid structures composed mainly of peptidoglycan, a mesh-like polymer that provides mechanical strength and maintains cell shape. The synthesis of peptidoglycan is a crucial process in bacterial growth and serves as a primary target for many antibiotics.Mechanism of Action of Beta-Lactam AntibioticsBeta-lactam antibiotics, such as penicillin, inhibit peptidoglycan synthesis in actively growing cells. These antibiotics share a characteristic four-membered...
01:25Inhibitors of Bacterial Protein Synthesis
Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
01:28Inhibitors of Bacterial DNA Synthesis
Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...
01:22Antiviral Nucleoside Inhibitors
Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...