Abstract
Background: The antimetabolite, 5-Fluorouracil (5-FU), is the only chemotherapeutic drug to significantly improve 12-month survival rates of patients with Colorectal Cancer (CRC). However, resistance to 5-FU is a major obstacle to effective treatment. The mechanism of 5-FU resistance has been discovered but is not fully known. Nuclear factor-erythroid 2-related factor 2 (Nrf2), a master regulator of cellular defense against oxidative and electrophilic stresses, is considered a major factor in 5-FU resistance.
Objective: The current study was conducted to discuss the role and mechanisms of Nrf2 in 5-FU resistance and to search for medicines or compounds that can reverse Nrf2-mediated 5-FU resistance.
Methods: Literature was obtained by defining specific search terms and searching several databases.
Results: Previous study suggested that overactivation of Nrf2 contributed to 5-FU resistance by regulating many cytoprotective genes. Interestingly, several medicines and compounds can repress 5-FU resistance mediated of Nrf2.
Conclusion: This review describes the major 5-FU-resistance mechanisms of Nrf2 and summarizes the medicines/ compounds that can overcome them.
Keywords: Colorectal Cancer (CRC), 5-Fluorouracil (5-FU), resistance, Nrf2, repress, medicine, compound.
Anti-Cancer Agents in Medicinal Chemistry
Title:Current Perspectives on the Role of Nrf2 in 5-Fluorouracil Resistance in Colorectal Cancer
Volume: 21 Issue: 17
Author(s): Jiayi Gong and Huaxi Xu*
Affiliation:
- School of Medicine, Jiangsu University, Zhenjiang 212013,China
Keywords: Colorectal Cancer (CRC), 5-Fluorouracil (5-FU), resistance, Nrf2, repress, medicine, compound.
Abstract:
Background: The antimetabolite, 5-Fluorouracil (5-FU), is the only chemotherapeutic drug to significantly improve 12-month survival rates of patients with Colorectal Cancer (CRC). However, resistance to 5-FU is a major obstacle to effective treatment. The mechanism of 5-FU resistance has been discovered but is not fully known. Nuclear factor-erythroid 2-related factor 2 (Nrf2), a master regulator of cellular defense against oxidative and electrophilic stresses, is considered a major factor in 5-FU resistance.
Objective: The current study was conducted to discuss the role and mechanisms of Nrf2 in 5-FU resistance and to search for medicines or compounds that can reverse Nrf2-mediated 5-FU resistance.
Methods: Literature was obtained by defining specific search terms and searching several databases.
Results: Previous study suggested that overactivation of Nrf2 contributed to 5-FU resistance by regulating many cytoprotective genes. Interestingly, several medicines and compounds can repress 5-FU resistance mediated of Nrf2.
Conclusion: This review describes the major 5-FU-resistance mechanisms of Nrf2 and summarizes the medicines/ compounds that can overcome them.
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Cite this article as:
Gong Jiayi and Xu Huaxi *, Current Perspectives on the Role of Nrf2 in 5-Fluorouracil Resistance in Colorectal Cancer, Anti-Cancer Agents in Medicinal Chemistry 2021; 21 (17) . https://dx.doi.org/10.2174/1871520621666210129094354
DOI https://dx.doi.org/10.2174/1871520621666210129094354 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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