Pharmacological Applications of Nrf2 Inhibitors as Potential Antineoplastic Drugs

• Published in: International journal of molecular sciences Vol. 20; no. 8; p. 2025
• Main Authors: Telkoparan-Akillilar, Pelin, Suzen, Sibel, Saso, Luciano
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 24.04.2019; MDPI
• Subjects: Activating transcription factor 3; Animals; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Antineoplastic drugs; Antioxidants; Apoptosis; Autoimmune diseases; BRG1 protein; cancer; cancer chemoprevention and therapy; Cancer therapies; Cell division; Cellular manufacture; chemoresistance; Chemotherapy; Clinical trials; Drug Development; Drugs; Enzymes; Estrogen receptors; Estrogens; Fra1 protein; Gene expression; Humans; Immune system; Immunotherapy; Kinases; Medical research; Neoplasms - drug therapy; Neoplasms - metabolism; NF-E2-Related Factor 2 - antagonists & inhibitors; NF-E2-Related Factor 2 - metabolism; Nrf2 inhibitors; Oxidants; Oxidative stress; Oxidative Stress - drug effects; Oxidizing agents; p53 Protein; Peroxisome proliferator-activated receptors; Precision medicine; Proteins; Retinoic acid; Retinoic acid receptors; Review; Signal Transduction - drug effects; Stem cells; Transcription factors; cancer chemoprevention and therapy; chemoresistance; Nrf2 inhibitors; cancer; antineoplastic drugs
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms20082025

Oxidative stress (OS) is associated with many diseases ranging from cancer to neurodegenerative disorders. Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) is one of the most effective cytoprotective controller against OS. Modulation of Nrf2 pathway constitutes a remarkable strategy in the antineoplastic treatments. A big number of Nrf2-antioxidant response element activators have been screened for use as chemo-preventive drugs in OS associated diseases like cancer even though activation of Nrf2 happens in a variety of cancers. Research proved that hyperactivation of the Nrf2 pathway produces a situation that helps the survival of normal as well as malignant cells, protecting them against OS, anticancer drugs, and radiotherapy. In this review, the modulation of the Nrf2 pathway, anticancer activity and challenges associated with the development of an Nrf2-based anti-cancer treatment approaches are discussed.