Treatment of diseases of oxidative stress through activation of the antioxidant nuclear factor E2-related factor 2 (NRF2) is limited by systemic side effects. We chemically functionalize the NRF2 activator monomethyl fumarate to require Baeyer–Villiger oxidation for release of the active drug at sites of oxidative stress. This prodrug reverses chronic pain in mice with reduced side effects and could be applied to other disorders of oxidative stress.

中文翻译：

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富马酸单甲酯的位点特异性药物释放治疗氧化应激障碍

通过激活抗氧化核因子 E2 相关因子 2 （NRF2） 来治疗氧化应激疾病受到全身副作用的限制。我们对 NRF2 激活剂富马酸单甲酯进行化学功能化，以需要 Baeyer-Villiger 氧化才能在氧化应激位点释放活性药物。这种前药可逆转小鼠的慢性疼痛，副作用减少，可应用于其他氧化应激疾病。