Therapeutic Targeting of the NRF2 Signaling Pathway in Cancer

Molecules

Dilek Cevik¹  Pelin Telkoparan-Akillilar¹  Sibel Suzen²  Luciano Saso³  Emiliano Panieri³ 

[1] Department of Medical Biology, Faculty of Medicine, Yuksek Ihtisas University, 06520 Ankara, Turkey;Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06560 Ankara, Turkey;Department of Physiology and Pharmacology, Faculty of Pharmacy and Medicine, “Vittorio Erspamer”, Sapienza University of Rome, 00185 Rome, Italy;

关键词: Nrf2;    Keap1;    cancer;    oxidative stress;   

DOI  :  10.3390/molecules26051417

来源: DOAJ

【 摘 要 】

Cancer is one of the most fatal diseases with an increasing incidence and mortality all over the world. Thus, there is an urgent need for novel therapies targeting major cancer-related pathways. Nuclear factor-erythroid 2-related factor 2 (NRF2) and its major negative modulator Kelch-like ECH-associated protein 1 (KEAP1) are main players of the cellular defense mechanisms against internal and external cell stressors. However, NRF2/KEAP1 signaling pathway is dysregulated in various cancers, thus promoting tumor cell survival and metastasis. In the present review, we discuss the mechanisms of normal and deregulated NRF2 signaling pathway focusing on its cancer-related functions. We further explore activators and inhibitors of this pathway as cancer targeting drug candidates in order to provide an extensive background on the subject.

【 授权许可】

Unknown