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Nrf2 抑制剂在抗肿瘤药物中的药理学应用。

Pharmacological Applications of Nrf2 Inhibitors as Potential Antineoplastic Drugs.

机构信息

Department of Medical Biology, Faculty of Medicine, Yuksek Ihtisas University, 06520 Balgat, Ankara, Turkey.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.

出版信息

Int J Mol Sci. 2019 Apr 24;20(8):2025. doi: 10.3390/ijms20082025.

Abstract

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.

摘要

氧化应激(OS)与许多疾病有关,从癌症到神经退行性疾病。核因子-红细胞 2 相关因子 2(Nrf2)是对抗 OS 的最有效细胞保护控制器之一。Nrf2 通路的调节构成了抗肿瘤治疗中的一种重要策略。已经筛选了大量的 Nrf2-抗氧化反应元件激活剂,用作 OS 相关疾病(如癌症)的化学预防药物,尽管 Nrf2 的激活发生在多种癌症中。研究证明,Nrf2 通路的过度激活会产生一种有助于正常和恶性细胞存活的情况,使它们免受 OS、抗癌药物和放疗的影响。在这篇综述中,讨论了 Nrf2 通路的调节、抗癌活性以及与基于 Nrf2 的抗癌治疗方法开发相关的挑战。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d0ff/6514836/b63b01466523/ijms-20-02025-g001.jpg

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