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|Ref Type||Journal Article|
|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.)|
|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.|
|Molecular Profile||Treatment Approach|
|Gene Name||Source||Synonyms||Protein Domains||Gene Description||Gene Role|
|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|