Description
Mechlorethamine is a nitrogen mustard DNA alkylator that binds and alkylates the N7 nitrogen on guanine and adenine bases in DNA. Mechlorethamine was initially developed as a blistering agent for use in chemical warfare but has since exhibited anticancer chemotherapeutic benefit. In vitro and in vivo, mechlorethamine forms a reactive aziridinium ion intermediate; it also can induce 5’-GNC-3’ DNA crosslinks. Additionally, this compound exhibits pro-oxidative activity, increasing levels of ROS and RNS in the treatment of B-cell chronic lymphocytic leukemia (CLL), inducing oxidative stress and apoptosis.
References
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Eder JP Jr, Chan VT, Ng SW, et al. DNA topoisomerase II alpha expression is associated with alkylating agent resistance. Cancer Res. 1995 Dec 15;55(24):6109-16. PMID: 8521401.
