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Antimalarial Drugs Induce the Selective Folding of Human Telomeric G-Quadruplex in a Cancer-Mimicking

Sunipa Sarkar1, Asim Bisoi1, Prashant Chandra Singh1

  • 1School of Chemical Sciences, Indian Association for the Cultivation of Science, Jadavpur, Kolkata 700032, India.

The Journal of Physical Chemistry. B
|July 19, 2023
PubMed

Insights

Antimalarial drugs show promise in cancer therapy by stabilizing G-quadruplex (Gq) DNA structures, particularly in cancer cell environments. Their effectiveness is region-specific, targeting telomere Gq over promoter Gq.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Therapeutics

Background:

  • G-quadruplex (Gq) DNA structures play a crucial role in regulating gene transcription, making them key targets for cancer therapy.
  • Antimalarial drugs are being investigated for cancer treatment, but their precise mechanisms of action, especially concerning Gq DNA, remain unclear.

Purpose of the Study:

  • To investigate the role of antimalarial drugs in folding and stabilizing G-quadruplex (Gq) DNA sequences.
  • To determine if antimalarial drugs exhibit selectivity towards Gq-forming DNA in telomere and promoter regions.
  • To assess the influence of different cellular microenvironments (cancerous vs. normal) on drug efficacy.

Main Methods:

  • Studied the folding and stabilization of Gq-forming DNA sequences from telomere and promoter regions.
  • Varied salt (KCl) concentrations to mimic in vitro cancerous and normal cell microenvironments.
  • Analyzed the interaction of antimalarial drugs with Gq DNA structures.

Main Results:

  • Antimalarial drugs preferentially fold and stabilize telomere Gq-forming sequences in a cancer cell microenvironment compared to promoter regions.
  • These drugs effectively promote Gq formation by preventing unfolding by complementary strands.
  • In normal cell microenvironments, potassium ions (K+) are the primary drivers of telomere folding, with a less prominent role for antimalarial drugs.

Conclusions:

  • The efficacy of antimalarial drugs in cancer therapy is dependent on the specific cellular microenvironment, showing higher activity in cancerous conditions.
  • Antimalarial drugs demonstrate selectivity for Gq-forming regions, particularly telomeric sequences.
  • This suggests a targeted therapeutic potential for antimalarial drugs in specific cancer types.

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