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ID: ALA3608247

Journal: Bioorg Med Chem Lett

Title: Human SIRT3 tripeptidic inhibitors containing N(ε)-thioacetyl-lysine.

Authors: Chen B, Wang J, Huang Y, Zheng W.

Abstract: Built upon our lead pan-SIRT1/2/3 tripeptidic inhibitors that contain the catalytic mechanism-based sirtuin inhibitory warhead N(ε)-thioacetyl-lysine, three of their analogs (i.e., 7, 9, and 19) were discovered in the current study to exhibit a significantly enhanced SIRT3 inhibitory selectivity while maintaining the SIRT3 inhibitory potency. These compounds represent novel lead compounds for developing more potent and selective SIRT3 inhibitors of the catalytic mechanism-based type.

CiteXplore: 26220157

DOI: 10.1016/j.bmcl.2015.07.008