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]
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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.