Description
Salermide is an inhibitor of sirtuins that exhibits anti-parasitic and anticancer chemotherapeutic activities. In Schistosoma mansoni, salermide decreases egg-laying activity, disrupts morphology of reproductive organs, and induces apoptosis and cell death. In breast cancer cells, salermide downregulates expression of sirtuin1, causing increases in p53 acetylation and cell death; additionally, salermide upregulates expression of DR5, ATF3, ATF4, and CHOP. Salermide also induces apoptosis in non-small cell lung cancer (NSCLC) cells) and inhibits tumor growth across a variety of animal models.
References
Lancelot J, Caby S, Dubois-Abdesselem F, et al. Schistosoma mansoni Sirtuins: characterization and potential as chemotherapeutic targets. PLoS Negl Trop Dis. 2013 Sep 12;7(9):e2428. PMID: 24069483.
Dastjerdi MN, Salahshoor MR, Mardani M, et al. The apoptotic effects of sirtuin1 inhibitor on the MCF-7 and MRC-5 cell lines. Res Pharm Sci. 2013 Apr;8(2):79-89. PMID: 24019817.
Liu G, Su L, Hao X, et al. Salermide up-regulates death receptor 5 expression through the ATF4-ATF3-CHOP axis and leads to apoptosis in human cancer cells. J Cell Mol Med. 2012 Jul;16(7):1618-28. PMID: 21801305.
Lara E, Mai A, Calvanese V, Altucci L, et al. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91. Erratum in: Oncogene. 2009 Feb 26;28(8):1168. Inhof, A [corrected to Imhof, A]. PMID: 19060927.
