925437-84-9Relevant articles and documents
Synthesis and Assay of SIRT1-Activating Compounds
Dai,Ellis,Sinclair,Hubbard
, p. 213 - 244 (2018/05/04)
The NAD+-dependent deacetylase SIRT1 plays key roles in numerous cellular processes including DNA repair, gene transcription, cell differentiation, and metabolism. Overexpression of SIRT1 protects against a number of age-related diseases including diabetes, cancer, and Alzheimer's disease. Moreover, overexpression of SIRT1 in the murine brain extends lifespan. A number of small-molecule sirtuin-activating compounds (STACs) that increase SIRT1 activity in vitro and in cells have been developed. While the mechanism for how these compounds act on SIRT1 was once controversial, it is becoming increasingly clear that they directly interact with SIRT1 and enhance its activity through an allosteric mechanism. Here, we present detailed chemical syntheses for four STACs, each from a distinct structural class. Also, we provide a general protocol for purifying active SIRT1 enzyme and outline two complementary enzymatic assays for characterizing the effects of STACs and similar compounds on SIRT1 activity.
Discovery of imidazo[1,2-6]thiazole derivatives as novel SIRT1 activators
Vu, Chi B.,Bemis, Jean E.,Disch, Jeremy S.,Ng, Pui Yee,Nunes, Joseph J.,Milne, Jill C.,Carney, David P.,Lynch, Amy V.,Smith, Jesse J.,Lavu, Siva,Lambert, Philip D.,Gagne, David J.,Jirousek, Michael R.,Schenk, Simon,Olefsky, Jerrold M.,Perni, Robert B.
experimental part, p. 1275 - 1283 (2009/12/07)
A series of imidazo[1,2-b]thiazole derivatives is shown to activate the NAD+-dependent deacetylase SIRT1, a potential new therapeutic target to treat various metabolic disorders. This series of compounds was derived from a high throughput scree
SIRTUIN MODULATING IMIDAZOTHIAZOLE COMPOUNDS
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Page/Page column 69; 71-72, (2009/01/23)
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.