articleProceedings of the National Academy of SciencesJan 4, 2011Closed access

Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism

DRDong‐Mei RenNVNicole VilleneuveTJTao JiangTWTongde WuALAlexandria Lau

University of Arizona · Shandong University

PubMed
Indexed incrossrefpubmed

Abstract

The major obstacle in cancer treatment is the resistance of cancer cells to therapies. Nrf2 is a transcription factor that regulates a cellular defense response and is ubiquitously expressed at low basal levels in normal tissues due to Keap1-dependent ubiquitination and proteasomal degradation. Recently, Nrf2 has emerged as an important contributor to chemoresistance. High constitutive expression of Nrf2 was found in many types of cancers, creating an environment conducive for cancer cell survival. Here, we report the identification of brusatol as a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells and A549 xenografts to cisplatin and other chemotherapeutic drugs.…

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648
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Authors

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Topics & keywords

Topics
Keywords
  • Cisplatin
  • Pharmacology
  • Ectopic expression
  • Cancer cell
  • A549 cell
  • Apoptosis
  • Chemistry
  • Cancer research
UN Sustainable Development Goals
  • Good health and well-being
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