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Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
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Related Experiment Video

Updated: Jul 7, 2026

Single-Molecule Fluorescence Visualization of DNA Polymerase Dynamics at G-Quadruplexes
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Published on: April 4, 2025

G-quadruplexes: targets in anticancer drug design.

Tian-miao Ou1, Yu-jing Lu, Jia-heng Tan

  • 1School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510080, People's Republic of China.

Chemmedchem
|February 1, 2008
PubMed
Summary

G-quadruplexes are DNA structures targeted by anticancer drugs. Improving drug selectivity for these structures is crucial to minimize side effects and enhance therapeutic efficacy.

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In Vitro Chemical Mapping of G-Quadruplex DNA Structures by Bis-3-Chloropiperidines

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Genetics

Background:

  • G-quadruplexes are unique secondary structures in guanine-rich DNA.
  • These structures are found in critical genomic regions like telomeres and gene regulatory elements.
  • G-quadruplexes are emerging targets for novel anticancer therapeutics.

Purpose of the Study:

  • To review research on G-quadruplexes as drug targets.
  • To provide insights into designing selective small-molecule ligands for G-quadruplexes.
  • To summarize methodologies for studying ligand-G-quadruplex interactions.

Main Methods:

  • Literature review of published research on G-quadruplexes.
  • Analysis of studies focusing on small-ligand binding to G-quadruplexes.
  • Compilation of research methodologies for G-quadruplex-ligand interaction studies.

Main Results:

  • G-quadruplexes play significant roles in biological regulation.
  • Several G-quadruplex-targeting compounds have advanced to clinical trials.
  • Current G-quadruplex-targeting anticancer drugs lack sufficient selectivity, leading to side effects.

Conclusions:

  • A clear understanding of G-quadruplex topology, biological roles, and ligand binding is essential for drug design.
  • Further research is needed to improve the selectivity of G-quadruplex-targeting anticancer agents.
  • This review offers valuable information for developing more effective and safer G-quadruplex-based therapies.