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Related Concept Videos

Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence the...
Inhibitors of Bacterial DNA Synthesis01:28

Inhibitors 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...
Conserved Binding Sites01:49

Conserved Binding Sites

Many proteins’ biological role depends on their interactions with their ligands, small molecules that bind to specific locations on the protein known as ligand-binding sites. Ligand-binding sites are often conserved among homologous proteins as these sites are critical for protein function.
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Single-Strand DNA Binding Proteins01:03

Single-Strand DNA Binding Proteins

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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Updated: Jun 7, 2026

Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers
08:28

Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers

Published on: September 19, 2017

Structure-based design of selective high-affinity telomeric quadruplex-binding ligands.

Caterina Maria Lombardo1, Iria Sánchez Martínez, Shozeb Haider

  • 1CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, London WC1N 1AX, UK.

Chemical Communications (Cambridge, England)
|November 2, 2010
PubMed
Summary
This summary is machine-generated.

Researchers created new triazole-based ligands that selectively bind to telomeric G-quadruplexes. These ligands were designed using computer modeling and structural data, showing promising binding affinities.

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Last Updated: Jun 7, 2026

Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers
08:28

Single-molecule Manipulation of G-quadruplexes by Magnetic Tweezers

Published on: September 19, 2017

Single-Molecule Fluorescence Visualization of DNA Polymerase Dynamics at G-Quadruplexes
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Single-Molecule Fluorescence Visualization of DNA Polymerase Dynamics at G-Quadruplexes

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Aptamer-Based Target Detection Facilitated by a 3-Stage G-Quadruplex Isothermal Exponential Amplification Reaction
03:38

Aptamer-Based Target Detection Facilitated by a 3-Stage G-Quadruplex Isothermal Exponential Amplification Reaction

Published on: October 6, 2022

Area of Science:

  • Medicinal Chemistry
  • Structural Biology
  • Biochemistry

Background:

  • Telomeric G-quadruplexes are unique DNA structures found at chromosome ends.
  • These structures are implicated in cellular processes and diseases, making them therapeutic targets.
  • Existing ligands, like tri-substituted acridines, show promise but can be further optimized.

Purpose of the Study:

  • To develop novel triazole-based ligands with selectivity for telomeric G-quadruplexes.
  • To design ligands that mimic the structural features of established acridine-based ligands.
  • To validate the design strategy through experimental assessment of binding affinities.

Main Methods:

  • Utilized crystal structure data of G-quadruplexes for computer-aided design.
  • Synthesized a library of triazole-based compounds.
  • Employed electrospray mass spectrometry to estimate ligand binding affinities.

Main Results:

  • Successfully developed a library of triazole-based ligands.
  • The ligands demonstrated selectivity for telomeric G-quadruplex structures.
  • Experimental binding affinities aligned with predictions from the computer-based design approach.

Conclusions:

  • The study successfully designed and synthesized novel triazole-based ligands targeting telomeric G-quadruplexes.
  • Computer-aided design based on structural data is an effective strategy for developing selective ligands.
  • The developed ligands represent a promising new class for G-quadruplex-related research and therapeutic development.