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Papers of the Week
Site-specific drug release of monomethyl fumarate to treat oxidative stress disorders.
Authors
Avery TD, Li J, Turner DJL, Rasheed MSU, Cherry FR, Stachura DL, Rivera-Escalera F, Ruiz DM, Lacagnina MJ, Gaffney CM, Aguilar C, Yu J, Wang Y, Xie H, Liang D, Shepherd AJ, Abell AD, Grace PMAbstract
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.