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Related Concept Videos

DNA Topoisomerases02:02

DNA Topoisomerases

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Topoisomerases are enzymes that relax overwound DNA molecules during various cell processes, including DNA replication and transcription. These enzymes regulate positive and negative DNA supercoiling without changing the nucleotide sequence. DNA overwinding in a clockwise direction results in positively supercoiled DNA, whereas underwinding in a counterclockwise direction produces negatively supercoiled DNA.
Types and Mechanism of action
Topoisomerases are divided into two main types. ...
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Gene Regulation in Microbial Communities: Quorum Sensing01:28

Gene Regulation in Microbial Communities: Quorum Sensing

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Quorum sensing is a mechanism of bacterial communication that enables coordinated gene expression in response to changes in population density. This facilitates collective behaviors that enhance survival, resource acquisition, and ecological adaptation. This process relies on small signaling molecules called autoinducers that accumulate as bacterial populations grow. When a critical threshold concentration of autoinducers is reached, bacterial cells collectively modify gene expression,...
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Development of Antibiotic Resistance01:30

Development of Antibiotic Resistance

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Antibiotic resistance is a major public health concern that arises when bacteria evolve mechanisms to withstand the effects of antibiotic treatments. This resistance can be intrinsic, acquired through genetic mutations, or transferred between bacteria via horizontal gene transfer. The development of antibiotic resistance poses significant challenges in treating bacterial infections and necessitates ongoing research to develop new therapeutic strategies.Intrinsic resistance occurs when bacterial...
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Genomic DNA in Prokaryotes00:46

Genomic DNA in Prokaryotes

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The genome of most prokaryotic organisms consists of double-stranded DNA organized into one circular chromosome in a region of cytoplasm called the nucleoid. The chromosome is tightly wound, or supercoiled, for efficient storage. Prokaryotes also contain other circular pieces of DNA called plasmids. These plasmids are smaller than the chromosome and often carry genes that confer adaptive functions, such as antibiotic resistance.
Genomic Diversity in Bacteria
Although bacterial genomes are much...
43.9K
DNA Helicases00:55

DNA Helicases

21.4K
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...
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Restriction Enzymes01:11

Restriction Enzymes

30.8K
Restriction enzymes are bacterial enzymes used to cut DNA in a sequence-specific manner. To cleave DNA, they bind to specific palindromic sequences called restriction sites. Such palindromic DNA sequences or inverted repeats are commonly found in regions of functional significance, such as the origin of replication, gene operator sites, and regions containing transcription termination signals.
The host bacteria protect their own genomic DNA from these enzymes by methylating these sites. Some...
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Related Experiment Video

Updated: Jul 12, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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Recent Development of DNA Gyrase Inhibitors: An Update.

Poonam Piplani1, Ajay Kumar1, Akanksha Kulshreshtha1

  • 1University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160017, India.

Mini Reviews in Medicinal Chemistry
|November 1, 2023
PubMed
Summary

Novel antimicrobial agents targeting DNA gyrase show promise in combating antibiotic resistance. This review explores new synthetic and natural inhibitors, including those in clinical trials, to overcome resistant bacterial and fungal infections.

Keywords:
DNA gyraseantimicrobialsmetal complexesmicrobes.nonfluoroquinolonesstructure-activity relationship

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Area of Science:

  • Microbiology
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Antimicrobial resistance (AMR) is a critical global health challenge, rendering existing treatments ineffective.
  • Bacterial and fungal infections persist and grow when standard drug regimens fail due to resistance.
  • Emerging resistance necessitates novel therapeutic strategies beyond conventional antibiotics like Ciprofloxacin and Novobiocin.

Purpose of the Study:

  • To review recent advancements in synthetic and natural DNA gyrase inhibitors.
  • To evaluate the potential of these agents in overcoming antimicrobial resistance.
  • To present information on molecules currently in clinical trials and their status.

Main Methods:

  • Literature review of synthetic and natural DNA gyrase inhibitors.
  • Analysis of Structure-Activity Relationships (SAR) for identified agents.
  • Examination of mechanisms of action for novel antimicrobial compounds.

Main Results:

  • Several novel synthetic and natural DNA gyrase inhibitors demonstrate significant potential against resistant microbes.
  • Agents targeting different sites on DNA gyrase, such as Zodiflodacin and Zenoxacin, have shown success.
  • Ongoing clinical trials are evaluating the efficacy and safety of promising new molecules.

Conclusions:

  • DNA gyrase remains a viable and crucial target for developing new antimicrobial agents.
  • Continued research into novel inhibitors is essential to combat the growing threat of antimicrobial resistance.
  • Understanding SAR and mechanisms of action will guide the design of more effective treatments.