1093403-37-2Relevant academic research and scientific papers
Search for a novel SIRT1 activator: Structural modification of SRT1720 and biological evaluation
Matsuya, Yuji,Kobayashi, Yuta,Uchida, Sayumi,Itoh, Yukihiro,Sawada, Hideyuki,Suzuki, Takayoshi,Miyata, Naoki,Sugimoto, Kenji,Toyooka, Naoki
, p. 4907 - 4910 (2013/09/02)
Syntheses and biological evaluation of novel SRT1720 derivatives are described in search for new candidates of SIRT1 activator. Several parts of the SRT1720 structure, including piperazine moiety, quinoxaline ring on the amide group, and position of the amide function, were modified, and the assay results indicated that transfer of the ortho amide-substituent regarding to the imidazo[1,2-b]thiazole core onto the meta position resulted in improvement of SIRT1 activation ability. Modeling analyses of SRT1720 and the most potent derivative bound to model complex of SIRT1 with peptide substrate were also performed.
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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, (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.
SIRTUIN POLYMORPHISMS AND METHODS OF USE THEREOF
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Page/Page column 35, (2008/12/08)
Provided herein are methods for diagnosis and prognosis using polymorphic variants of sirtuins. Such polymorphic may be used, for example, to identify subjects that would be responsive to treatment with a sirtuin modulating compound andor subjects that are suffering from or susceptible to a disease mediated by a sirtuin. Also provided are methods for determining the predictive value of a sirtuin polymorphic variant, methods for evaluating sirtuin modulating compounds, and methods for determining appropriate dosage andor treatment regimens for subjects having one or more sirtuin polymorphic variants. Screening methods for identifying sirtuin modulating compounds using polymorphic variants of a sirtuin are also provided.
