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.
摘要译文
癌症是世界各地发病率和死亡率越来越大的致命疾病之一。因此，迫切需要针对主要癌症相关途径的新疗法。核因子 - 红细胞2相关因子2（NRF2）及其主要的阴性调节剂kelch样eqh-ery蛋白1（Keap1）是针对内部和外部细胞压力源的细胞防御机制的主要球员。然而，NRF2 / Keap1信号传导途径在各种癌症中进行了失调，从而促进肿瘤细胞存活和转移。在本综述中，我们讨论了重点在其癌症相关功能上的正常和解毒的NRF2信号传导途径的机制。我们进一步探索该途径的活化剂和抑制剂作为癌症靶向毒品候选者，以便为受试者提供广泛的背景。
Pelin Telkoparan-Akillilar[ 1]; Emiliano Panieri[ 2]; Dilek Cevik[ 1]; Sibel Suzen[ 3];Luciano Saso[ 2;[*]. Therapeutic Targeting of the NRF2 Signaling Pathway in Cancer[J]. Molecules, 2021,26(5): 1417