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Quadruplex Ligands in Cancer Therapy.

Victoria Sanchez-Martin1,2,3, Miguel Soriano1,4, Jose Antonio Garcia-Salcedo1,2

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Quadruplex structures in DNA and RNA are crucial in biological processes and cancer. This review explores small molecules targeting these structures for cancer therapy.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Genetics

Background:

  • Nucleic acids form non-canonical four-stranded structures called quadruplexes.
  • G-quadruplexes (guanine-rich) and i-Motifs (cytosine-rich) are found in human DNA and RNA.
  • These structures are implicated in critical cellular functions including gene regulation and genome stability.

Purpose of the Study:

  • To review and consolidate current literature on quadruplex ligands in cancer therapy.
  • To categorize ligands targeting DNA G-quadruplexes, RNA G-quadruplexes, and DNA i-Motifs.
  • To highlight the therapeutic potential of targeting quadruplex structures in oncology.

Main Methods:

  • Literature review and synthesis of existing research.
  • Categorization of small-molecule ligands based on their target quadruplex structures (DNA G4, RNA G4, i-Motifs).
  • Analysis of the role of quadruplexes in cancer biology and their therapeutic targeting.

Main Results:

  • Quadruplexes play significant roles in the biology of oncogenes, tumor suppressors, telomeres, and genome instability.
  • Numerous small-molecule ligands targeting DNA and RNA quadruplexes have been identified.
  • These ligands show promise as potential anticancer agents by modulating quadruplex structures.

Conclusions:

  • Quadruplex structures represent a promising frontier for cancer drug development.
  • Targeting DNA and RNA quadruplexes with small molecules offers a novel therapeutic strategy.
  • Further research into quadruplex ligands could lead to new cancer treatments.