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Ref Type Journal Article
PMID (25486469)
Authors Wilking MJ, Singh CK, Nihal M, Ndiaye MA, Ahmad N
Title Sirtuin deacetylases: a new target for melanoma management.
Journal Cell cycle (Georgetown, Tex.)
Vol 13
Issue 18
Date 2014
URL
Abstract Text Melanoma continues to cause more deaths than any other skin cancer, necessitating the development of new avenues of treatment. One promising new opportunity comes in the form of mechanism-based therapeutic targets. We recently reported the overexpression and delocalization of the class III histone deacetylase SIRT1 in melanoma, and demonstrated that its small molecule inhibition via Tenovin-1 decreased cell growth and viability of melanoma cells, possibly by a p53 mediated induction of p21. Here, we support our data using additional SIRT inhibitors, viz. Sirtinol and Ex-527, which suggests possible benefits of concomitantly inhibiting more than one Sirtuin for an effective cancer management strategy. This "Extra View" paper also includes a discussion of our results in the context of similar recent and concurrent studies. Furthermore, we expand upon our findings in an analysis of new research that may link the cellular localization and growth effects of SIRT1 with the PI3K signaling pathway.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
EX-527 EX-527 1 0
Sirtinol Sirtinol 1 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
EX-527 EX 527|Selisistat SIRT1 Inhibitor 5 SIRT2 Inhibitor 5 SIRT3 Inhibitor 1 Selisistat (EX-527) inhibits SIRT1, SIRT2, and SIRT3, potentially resulting in decreased tumor cell growth (PMID: 25486469, PMID: 32711231).
Sirtinol SIRT1 Inhibitor 5 SIRT2 Inhibitor 5 Sirtinol inhibits SIRT1 and SIRT2, with higher activity towards SIRT2, which may result in decreased tumor cell growth (PMID: 25486469, PMID: 32377734).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown melanoma not applicable EX-527 Preclinical Actionable In a preclinical study, Ex-527 inhibited growth of human melanoma cell lines in culture (PMID: 25486469). 25486469
Unknown unknown melanoma not applicable Sirtinol Preclinical Actionable In a preclinical study, Sirtinol inhibited growth of human melanoma cell lines in culture (PMID: 25486469). 25486469