NQO1 Inhibitors

NQO1 inhibitors belong to a class of chemical compounds designed to modulate the activity of NAD(P)H quinone oxidoreductase 1 (NQO1), an enzyme involved in cellular detoxification and antioxidant defense mechanisms. NQO1 plays a pivotal role in protecting cells from oxidative stress by catalyzing the reduction of quinones and other substrates, preventing the generation of reactive oxygen species (ROS) and harmful oxidative compounds. Additionally, NQO1 participates in the activation and stabilization of certain anticancer drugs and functions as a cytoprotective enzyme against electrophilic and redox-cycling compounds. Its role in detoxification processes is critical for cellular health and defense against oxidative damage. Inhibitors targeting NQO1 aim to interfere with its enzymatic activity, often by binding to specific regions on the enzyme or altering its structural conformation, thereby impeding its ability to catalyze the reduction of quinones and other substrates. By inhibiting NQO1, these compounds disrupt the cellular defense mechanisms against oxidative stress and interferes with the activation or detoxification of certain drugs metabolized by NQO1. This disruption may lead to an accumulation of reactive species and altered cellular redox balance, impacting various cellular processes beyond detoxification pathways.