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An update of Nrf2 activators and inhibitors in cancer prevention/promotion

Farhad Pouremamali, Amir Pouremamali, Mehdi Dadashpour, Narges Soozangar, Farhad Jeddi

2022Cell Communication and Signaling178 citationsDOIOpen Access PDF

Abstract

NF-E2-related factor 2 (Nrf2) protein is a basic-region leucine zipper transcription factor that defends against endogenous or exogenous stressors. By inducing several cytoprotective and detoxifying gene expressions, Nrf2 can increase the sensitivity of the cells to oxidants and electrophiles. Transient Nrf2 activation, by its specific activators, has protective roles against carcinogenesis and cancer development. However, permanent activation of Nrf2 promotes various cancer properties, comprising malignant progression, chemo/radio resistance, and poor patient prognosis. Taken together, these findings suggest that reaching an optimal balance between paradoxical functions of Nrf2 in malignancy may render a selective improvement to identify therapeutic strategies in cancer treatment. In this review, we describe lately discovered Nrf2 inducers and inhibitors, and their chemopreventive and/or anticancer activities.

Topics & Concepts

Transcription factorCancer researchCarcinogenesisCancerTumor promotionEndogenyCancer cellCancer preventionMedicineBioinformaticsPharmacologyBiologyGeneInternal medicineBiochemistryGenomics, phytochemicals, and oxidative stressGlutathione Transferases and PolymorphismsRedox biology and oxidative stress
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