Description
Tenovin-6 is an inhibitor of sirtuins 1 and 2 (SIRT1/2) that also indirectly activates p53; sirtuins are considered class III histone deacetylases (HDACs). Tenovin-6 exhibits anticancer chemotherapeutic activity in several models. In chronic lymphocytic leukemia (CLL) cells, tenovin-6 increases levels of LC3-II and p62, dysregulating autophagy. In colon cancer cells, this compound increases levels of death receptor 5 (DR5), inducing apoptosis. Tenovin-6 also decreases tumor growth in animal models.
References
Ueno T, Endo S, Saito R, et al. The sirtuin inhibitor tenovin-6 upregulates death receptor 5 and enhances cytotoxic effects of 5-Fluorouracil and oxaliplatin in colon cancer cells. Oncol Res. 2014;21(3):155-64. PMID: 24512730.
MacCallum SF, Groves MJ, James J, et al. Dysregulation of autophagy in chronic lymphocytic leukemia with the small-molecule Sirtuin inhibitor Tenovin-6. Sci Rep. 2013;3:1275. PMID: 23429453.
Lain S, Hollick JJ, Campbell J, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. PMID: 18455128.
Brooks CL, Gu W. p53 Activation: a case against Sir. Cancer Cell. 2008 May;13(5):377-8. PMID: 18455119.
