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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.
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For successful DNA replication, the unwinding of double-stranded DNA must be accompanied by stabilization and protection of the separated single strands of the DNA. This crucial task is performed by single-strand DNA-binding (SSB) proteins. They bind to the DNA in a sequence-independent manner, which means that the nitrogenous bases of the DNA need not be present in a specific order for binding of SSB proteins to it. The binding of SSB proteins straightens single-stranded DNA (ssDNA) and makes...
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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,
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Nucleic Acid Structure01:25

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The pentose sugar in DNA is deoxyribose, while in RNA the pentose sugar is ribose. The difference between the sugars is the presence of the hydroxyl group on the ribose's second carbon and a hydrogen on the deoxyribose's second carbon. The phosphate residue attaches to the hydroxyl group of the 5′ carbon of one sugar and the hydroxyl group of the 3′ carbon of the sugar of the next nucleotide, which forms  a 5′ to 3′ phosphodiester linkage.
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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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The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
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Updated: Jun 27, 2025

Author Spotlight: Characterizing DNA G-Quadruplex by Bis-3-Chloropiperidine Based Chemical Mapping
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Amodiaquine Nonspecifically Binds Double Stranded and Three-Way Junction DNA Structures.

Sladjana Slavkovic1, Aron A Shoara1, Yunus A Kaiyum1

  • 1Department of Chemistry, York University, 4700 Keele St., Toronto, Ontario, Canada, M3J 1P3.

Chembiochem : a European Journal of Chemical Biology
|April 26, 2024
PubMed
Summary

Antimalarial drugs like amodiaquine and chloroquine bind DNA. Amodiaquine strongly binds double-stranded DNA, while other antimalarials show weaker interactions, offering new insights for drug development.

Keywords:
DNA structureITCamodiaquineantimalarialsaptamer

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • The 4-aminoquinoline class, including amodiaquine and chloroquine, are vital antimalarial drugs.
  • Their precise mechanism of action, particularly DNA interaction, remains largely unknown.

Purpose of the Study:

  • To investigate the DNA-binding affinities of amodiaquine, chloroquine, quinine, and mefloquine.
  • To explore the range of nucleic acid structures these compounds interact with.

Main Methods:

  • Isothermal titration calorimetry (ITC) for high-affinity binding (nM to tens of μM).
  • Nuclear Magnetic Resonance (NMR) spectroscopy for low-affinity binding (hundreds of μM).
  • Free energy binding simulations using the Dickerson-Drew dodecamer.

Main Results:

  • Amodiaquine demonstrated tight binding across all tested double-stranded DNA structures.
  • Mefloquine exhibited strong binding to DNA duplexes and weak binding to a three-way junction.
  • Quinine and chloroquine showed only weak binding to DNA duplexes.

Conclusions:

  • Differential DNA binding affinities among 4-aminoquinoline antimalarials revealed.
  • Findings provide a basis for understanding antimalarial activity and developing novel therapeutics.