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Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Baicalein Sensitizes Radioresistant BT549 and MCF7-R Breast Cancer Cells by Modulating Rac1 Signaling.

Zitong Zhao1, Zhangyun Li2, Quanzhou Peng3

  • 1The Comprehensive Breast Care Center, the Second Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi, People's Republic of China.

Phytotherapy Research : PTR
|June 2, 2026
PubMed
Summary
This summary is machine-generated.

Baicalein, a natural compound, enhances breast cancer radiosensitivity by inhibiting Rac1 activity and delaying DNA repair. This discovery offers a new therapeutic strategy to combat radioresistant breast cancer.

Keywords:
Rac1baicaleinbreast cancerradioresistance

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Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Radioresistance is a significant challenge in breast cancer (BC) treatment.
  • Baicalein, a flavonoid, has demonstrated potential in improving radiosensitivity.

Purpose of the Study:

  • To investigate the efficacy of baicalein as a radiosensitizer in breast cancer models.
  • To elucidate the underlying molecular mechanisms of baicalein's radiosensitizing effects, focusing on Rac1.

Main Methods:

  • Establishment and validation of radioresistant breast cancer cell models.
  • Assessment of radiosensitizing effects using clonogenic survival and DNA damage assays (γ-H2AX foci, neutral comet).
  • Identification of Rac1 as a key mediator through bioinformatics and interaction analyses.
  • Molecular docking, molecular dynamics (MD) simulations, and Surface Plasmon Resonance (SPR) to evaluate baicalein-Rac1 interaction.
  • In vitro and in vivo studies (xenografts) to assess Rac1 inhibition and therapeutic effects.

Main Results:

  • Baicalein significantly enhanced radiosensitivity in BT549 and MCF7-R breast cancer cells.
  • Baicalein inhibited Rac1 activity, leading to delayed DNA repair via the NHEJ pathway.
  • Molecular simulations confirmed strong binding affinity and stable interaction between baicalein and Rac1.
  • In vivo studies demonstrated Rac1 pathway inhibition, reduced tumor growth, and enhanced radiosensitivity.
  • High Rac1 expression correlated with poorer clinical outcomes in breast cancer patients.

Conclusions:

  • Baicalein acts as a potent radiosensitizer in breast cancer by inhibiting Rac1 activity and impairing DNA repair.
  • The findings suggest baicalein as a promising therapeutic agent to overcome radioresistance in breast cancer.
  • Targeting the Rac1 pathway with baicalein presents a novel strategy for improving breast cancer treatment efficacy.