Piperlongumine
Glutathione sponge / Increases ROS levels / Elevates cellular levels of reactive oxygen species selectively in cancer cell lines1. Irreversible glutathionylation leading to depletion of cellular glutathione is associated with its cellular toxicity2. Piperlongamine does not appear to have any effect on normal cells. Displays anti-tumor effects in a mouse xenograft tumor model as well as in spontaneously formed malignant breast tumors in mice1. Elevation of ROS levels may be due to inhibition of ubiquitin-proteasome system at a pre-proteasomal step.3
Biochemicals & reagents
20069-09-4
1) Raj et al. (2011), Selective killing of cancer cells by a small molecule targeting the stress response to ROS.; Nature, 475 7355. / 2) Adams et al. (2012), Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs.; Proc. Natl. Acad. Sci. USA, 109 15115 / Jarvius et al. (2013), Piperlongumine induces inhibition of the ubiquitin-proteasome system in cancer cells; Biochem. Biophys. Res. Commun. 10.1016/j.bbrc.2013.01.017
RT
TARGET: Glutathione -- PATHWAY: Redox; Senescence -- RESEARCH AREA: Ubiquitin/Proteasome; Oxidative stress -- DISEASE AREA: Cancer