Target Validation Information
TTD ID	T14731
Target Name	NAD-dependent deacetylase sirtuin-1 (SIRT1)
Type of Target	Clinical trial
Drug Potency against Target	2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide	Drug Info	IC50 = 3300 nM	[2]
	2H-chromeno[2,3-d]pyrimidine-2,4(3H)-dione	Drug Info	IC50 = 5300 nM	[4]
	Para-sirtinol	Drug Info	IC50 = 13000 nM	[1]
	Ro31-8220	Drug Info	IC50 = 5100 nM	[3]
Action against Disease Model	Resveratrol	Drug Info	Resveratrol (100-150 microM) exhibited anti-proliferative properties in HT-29 cells even after IGF-1 exposure by arresting G0/G1-S phase cell cycle progression through p27 stimulation and cyclin D1 suppression. Treatment with resveratrol suppressed IGF-1R protein levels and concurrently attenuated the downstream Akt/Wnt signaling pathways that play a critical role in cell proliferation.	[5]
References
REF 1	Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors. J Med Chem. 2005 Dec 1;48(24):7789-95.
REF 2	Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54.
REF 3	Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. J Med Chem. 2006 Dec 14;49(25):7307-16.
REF 4	Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specif... J Med Chem. 2010 Feb 11;53(3):1407-11.
REF 5	Resveratrol suppresses IGF-1 induced human colon cancer cell proliferation and elevates apoptosis via suppression of IGF-1R/Wnt and activation of p53 signaling pathways. BMC Cancer. 2010 May 26;10:238.

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