A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer

Abstract

Background: Pharmacological inhibition of the NAD--dependent deacetylase SIRT2 holds promise for cancer therapy by preventing deacetylation and inactivation of p53. Results: We identified two novel SIRT2 inhibitors that induce apoptosis in a p53-dependent fashion and activate three p53 target genes. Conclusion: Small-molecule inhibition of SIRT2 activates p53-dependent apoptosis in cancer cells. Significance: The compounds reported here are promising lead candidates for use in cancer treatment. © 2014 by The American Society for Biochemistry and Molecular Biology, Inc.