SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively). In diet-induced obese and diabetic leptin-deficient ob/ob mice, oral administration of 100 mg/kg SRT1720 once daily improves insulin sensitivity, lowers plasma glucose and increases mitochondrial capacity after one week of treatment[1]. SRT 1720 effectively decreases the acetylation of p53 in cells even in the absence of SIRT1, and this is attributed to inhibition of histone acetyltransferase p300[2].
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