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Microtubule-Targeting NAP Peptide-Ru(II)-polypyridyl Conjugate As a Bimodal Therapeutic Agent for Triple Negative

Atin Chatterjee1,2, Sandip Sarkar1, Sangheeta Bhattacharjee3

  • 1Department of Chemical Sciences and Center for Advanced Functional Materials, Indian Institute of Science Education and Research (IISER) Kolkata, Mohanpur 741246, West Bengal, India.

Journal of the American Chemical Society
|December 26, 2024
PubMed

Insights

A novel Ru-NAP photosensitizer effectively treats triple-negative breast cancer (TNBC) by targeting microtubules and utilizing photodynamic therapy. This conjugate shows enhanced binding affinity and potent anti-cancer activity in vitro and in vivo.

Area of Science:

  • Biochemistry
  • Materials Science
  • Oncology

Background:

  • Triple-negative breast cancer (TNBC) presents significant therapeutic challenges due to its aggressive nature and lack of targeted therapies.
  • Developing novel photosensitizers for combined chemotherapy and photodynamic therapy (PDT) is crucial for improving TNBC treatment outcomes.

Purpose of the Study:

  • To synthesize and characterize a novel Ru-NAP photosensitizer for targeted TNBC treatment.
  • To evaluate the efficacy of Ru-NAP in vitro and in vivo, leveraging microtubule disruption and PDT.

Main Methods:

  • Covalent coupling of an octapeptide (NAP) to a Ruthenium tris(2,2'-bipyridine) derivative (Rubpy) to form the Ru-NAP conjugate.
  • Assessment of Ru-NAP's binding affinity to β-tubulin using biophysical methods and computational docking.
  • Evaluation of Ru-NAP's cytotoxicity, cell cycle arrest, apoptosis induction, and tumor growth inhibition in TNBC models (MDA-MB-231) and control cells (HEK293).

Main Results:

  • Ru-NAP exhibited enhanced molecular aggregation and significantly higher binding affinity to β-tubulin compared to NAP alone, attributed to electrostatic interactions.
  • Ru-NAP demonstrated selective toxicity towards TNBC cells over HEK293 cells upon light exposure, with potent inhibition of cell proliferation and induction of apoptosis.
  • In vivo studies showed that Ru-NAP effectively inhibited tumor growth in MDA-MB-231 xenograft models.

Conclusions:

  • The Ru-NAP conjugate is a promising photosensitizer with dual-action therapeutic potential against TNBC.
  • Ru-NAP's ability to target microtubules and induce PDT offers a novel strategy for TNBC treatment, showing superior efficacy and selectivity.

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