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Updated: Jan 6, 2026

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Bimodular Antiparallel G-Quadruplex Nanoconstruct with Antiproliferative Activity.

Olga Antipova1, Nadezhda Samoylenkova2, Ekaterina Savchenko3

  • 1Chemistry Department, Lomonosov Moscow State University, Leninskiye Gory 1-40, 119991 Moscow, Russia. antipovachem@gmail.com.

Molecules (Basel, Switzerland)
|October 11, 2019
PubMed
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New DNA structures called biHD1 show antiproliferative activity against cancer cells. This discovery opens doors for designing novel G-quadruplex (GQ) nanoconstructs for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Nanotechnology

Background:

  • Oligonucleotides with antiproliferative activity are crucial in cancer research.
  • G-quadruplex (GQ) structures are a key feature of many anticancer oligonucleotides.
  • The DNA oligonucleotide HD1, a minimal GQ, demonstrates antiproliferative effects on cancer cells.

Purpose of the Study:

  • To analyze the antiproliferative activities of a novel bimodular DNA oligonucleotide, biHD1.
  • To investigate the structure-activity relationship of biHD1 derivatives in cancer cell lines.
  • To explore the potential of multimodular GQ nanoconstructs for cancer treatment.

Main Methods:

  • Synthesis and characterization of the biHD1 oligonucleotide.
  • Evaluation of antiproliferative activity using MTT assays.
Keywords:
DNA G-quadruplex oligonucleotideantiproliferative activityhuman cancer cell linesnanoconstruct

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  • Assessment of proliferation inhibition via Ki-67 immunoassay.
  • Structure-activity relationship studies on biHD1 derivatives.

    • Main Results:

    • BiHD1 exhibits dose-dependent antiproliferative activity against RL-67 (lung cancer) and U87 (central nervous system cancer) cell lines.
    • A correlation between G-quadruplex folding and antiproliferative efficacy was identified for biHD1 derivatives.
    • The covalent linkage of two GQ modules in biHD1 enhances the antiproliferative potential.

    Conclusions:

    • The biHD1 oligonucleotide demonstrates significant antiproliferative activity, validating the design strategy.
    • Covalently linked GQ modules offer a promising approach for developing novel anticancer agents.
    • This study paves the way for designing multimodular GQ nanoconstructs as therapeutic agents or drug carriers.