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Design and development of Nrf2 modulators for cancer chemoprevention and therapy: a review

Authors Sova M, Saso L

Received 29 April 2018

Accepted for publication 10 July 2018

Published 25 September 2018 Volume 2018:12 Pages 3181—3197

DOI https://doi.org/10.2147/DDDT.S172612

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Professor Jianbo Sun


Matej Sova,1 Luciano Saso2

1Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia; 2Department of Physiology and Pharmacology “Vittorio Erspamer”, Sapienza University, Rome, Italy

Abstract: A major cell defense mechanism against oxidative and xenobiotic stress is mediated by the Nrf2/Keap1 signaling pathway. The Nrf2/Keap1 pathway regulates gene expression of many cytoprotective and detoxifying enzymes, thus playing a pivotal role in maintaining redox cellular homeostasis. Many diseases including cancer have been closely related to impaired Nrf2 activity. Targeting Nrf2 and modulating its activity represents a novel modern strategy for cancer chemoprevention and therapy. In this review, different design strategies used for the development of Nrf2 modulators are described in detail. Moreover, the main focus is on important and recently developed Nrf2 activators and inhibitors, their in vitro and in vivo studies, and their potential use as chemopreventive agents and/or cancer therapeutics.

Keywords: Nrf2, oxidative stress, signaling pathway, cytoprotective, chemopreventive agents, cancer therapeutics

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