Department of Medical Biotechnology, Faculty of Advanced Medical Sciences, Tabriz University of Medical Sciences, Tabriz, Iran.
Department of Virology, Faculty of Medical Sciences, Tarbiat Modares University, Tehran, Iran.
Cell Commun Signal. 2022 Jun 30;20(1):100. doi: 10.1186/s12964-022-00906-3.
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.
核因子红细胞 2 相关因子 2(Nrf2)蛋白是一种碱性亮氨酸拉链转录因子,可抵御内源性或外源性应激源。通过诱导几种细胞保护和解毒基因的表达,Nrf2 可以提高细胞对氧化剂和亲电物的敏感性。其特定激活剂的 Nrf2 短暂激活在致癌作用和癌症发展中具有保护作用。然而,Nrf2 的永久激活促进了各种癌症特性,包括恶性进展、化疗/放疗耐药和患者预后不良。综上所述,这些发现表明,在恶性肿瘤中 Nrf2 的矛盾功能之间达到最佳平衡,可能会选择性地改善癌症治疗的治疗策略。在这篇综述中,我们描述了最近发现的 Nrf2 诱导剂和抑制剂及其化学预防和/或抗癌活性。