Small molecule activators of SIRT1 replicate signaling pathways triggered by calorie restriction in vivoJesse J Smith
Sirtris, a GSK Company, 200 Technology Square, Cambridge, MA 02139, USA
BMC Syst Biol 3:31. 2009
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Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activatorsChi B Vu
Sirtris Pharmaceuticals, Cambridge, Massachusetts 02139, USA
J Med Chem 52:1275-83. 2009
..The most potent analogue within this series, namely, compound 29, has demonstrated oral antidiabetic activity in the ob/ob mouse model, the diet-induced obesity (DIO) mouse model, and the Zucker fa/fa rat model...
- Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
Jean E Bemis
Sirtris, a GSK Company, Cambridge, MA 01239, USA
Bioorg Med Chem Lett 19:2350-3. 2009
..Herein, we describe the identification and SAR of a series of oxazolo[4,5-b]pyridines as novel small molecule activators of SIRT1 which are structurally unrelated to and more potent than resveratrol...
- A687V EZH2 is a gain-of-function mutation found in lymphoma patients
Christina R Majer
Epizyme, Inc, 325 Vassar St, Cambridge, MA 02139, USA
FEBS Lett 586:3448-51. 2012
..We propose that A687V EZH2 also leads to hypertrimethylation of H3K27 and may thus be a driver mutation in NHL...
- Biochemical characterization, localization, and tissue distribution of the longer form of mouse SIRT3
Lei Jin
Sirtris, a GSK Company, 200 Technology Square, Cambridge, MA 02139, USA
Protein Sci 18:514-25. 2009
..Thus, identification and characterization of the actual SIRT3 sequence should help resolve the debate about the nature of mouse SIRT3 and identify new mechanisms to modulate enzymatic activity...
- Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes
Jill C Milne
Sirtris Pharmaceuticals Inc, 790 Memorial Drive, Cambridge, Massachusetts 02139, USA
Nature 450:712-6. 2007
..Thus, SIRT1 activation is a promising new therapeutic approach for treating diseases of ageing such as type 2 diabetes...
- Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor
Scott R Daigle
Epizyme, Inc, Cambridge, MA 02139, USA
Cancer Cell 20:53-65. 2011
..Finally, in vivo administration of EPZ004777 leads to extension of survival in a mouse MLL xenograft model. These results provide compelling support for DOT1L inhibition as a basis for targeted therapeutics against MLL...
