Mingjuan Zhang, Yaping Jing, Qingbin Cui
Dimethyl fumarate (DMF) is an approved medication by the FDA for the treatment of multiple sclerosis, primarily targeting and regulating the NF-κB pathway. Recently, its anticancer effects have drawn considerable attention as it not only effectively kills a panel of different cancer cells in vitro and in vivo , but also synergizes with other conventional or targeted chemotherapeutics in certain resistant or refractory cancer cells. Mechanism studies showed that in addition to inhibiting NF-κB and stimulating Nrf2, DMF functioned as a chemotherapy also by suppressing inflammation, inhibiting epigenetic modifications, as well as modulating epithelial-mesenchymal transition (EMT). On the molecular level, DMF can form a covalent bond with the thiol group of a protein. In this paper, we provide a brief review of the anticancer studies of DMF, either as a single agent or in combination regimens. While DMF is a relatively weak cytotoxic agent, it is effective in sensitizing cells to other chemotherapeutic agents. Since DMF is already an approved drug, its fast-track approval for cancers may bring new hope to those chemo-resistant patients who suffer from very limited treatment options.